Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
90469674 178601 7 None 3 3 Rat 10.7 pEC50 = 10.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4468523 178601 7 None 3 3 Rat 10.7 pEC50 = 10.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
2181 8113 42 None 6 4 Rat 10.5 pEC50 = 10.5 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00132
2182 8113 42 None 6 4 Rat 10.5 pEC50 = 10.5 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00132
27991 8113 42 None 6 4 Rat 10.5 pEC50 = 10.5 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00132
5311065 8113 42 None 6 4 Rat 10.5 pEC50 = 10.5 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00132
CHEMBL1429 8113 42 None 6 4 Rat 10.5 pEC50 = 10.5 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00132
CHEMBL264448 8113 42 None 6 4 Rat 10.5 pEC50 = 10.5 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00132
DB00035 8113 42 None 6 4 Rat 10.5 pEC50 = 10.5 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00132
44419026 175278 17 None 478 3 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL435323 175278 17 None 478 3 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
2168 10748 38 None -12 6 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL None None None None 10.1021/jm200278m
2810 10748 38 None -12 6 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL None None None None 10.1021/jm200278m
644077 10748 38 None -12 6 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL None None None None 10.1021/jm200278m
CHEMBL373742 10748 38 None -12 6 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL None None None None 10.1021/jm200278m
DB00067 10748 38 None -12 6 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL None None None None 10.1021/jm200278m
118476355 180643 3 None 5 3 Rat 10.3 pEC50 = 10.3 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4539370 180643 3 None 5 3 Rat 10.3 pEC50 = 10.3 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
2168 10748 38 None -12 6 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL None None None None 10.1021/jm200278m
2810 10748 38 None -12 6 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL None None None None 10.1021/jm200278m
644077 10748 38 None -12 6 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL None None None None 10.1021/jm200278m
CHEMBL373742 10748 38 None -12 6 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL None None None None 10.1021/jm200278m
DB00067 10748 38 None -12 6 Human 10.3 pEC50 = 10.3 Functional
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
ChEMBL None None None None 10.1021/jm200278m
2168 10748 38 None -12 6 Human 10.3 pEC50 = 10.3 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL None None None None 10.1016/j.bmcl.2005.10.107
2810 10748 38 None -12 6 Human 10.3 pEC50 = 10.3 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL None None None None 10.1016/j.bmcl.2005.10.107
644077 10748 38 None -12 6 Human 10.3 pEC50 = 10.3 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL None None None None 10.1016/j.bmcl.2005.10.107
CHEMBL373742 10748 38 None -12 6 Human 10.3 pEC50 = 10.3 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL None None None None 10.1016/j.bmcl.2005.10.107
DB00067 10748 38 None -12 6 Human 10.3 pEC50 = 10.3 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL None None None None 10.1016/j.bmcl.2005.10.107
90469674 178601 7 None -3 3 Human 10.2 pEC50 = 10.2 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4468523 178601 7 None -3 3 Human 10.2 pEC50 = 10.2 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
155523986 177689 0 None 724 3 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4454891 177689 0 None 724 3 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
90469608 179039 0 None 812 2 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4474518 179039 0 None 812 2 Human 10.1 pEC50 = 10.1 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476384 177652 0 None 1778 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4454160 177652 0 None 1778 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
90469675 178196 0 None 1412 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4462743 178196 0 None 1412 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476338 180170 0 None 2290 3 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4528032 180170 0 None 2290 3 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476337 180368 0 None 1584 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4533159 180368 0 None 1584 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476357 182369 0 None 2630 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4579754 182369 0 None 2630 2 Human 10.0 pEC50 = 10 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476361 180514 0 None 363 2 Human 10.0 pEC50 = 10.0 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4536454 180514 0 None 363 2 Human 10.0 pEC50 = 10.0 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476343 180876 0 None 1174 2 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4544907 180876 0 None 1174 2 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476360 180341 0 None 2691 2 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4532363 180341 0 None 2691 2 Human 9.9 pEC50 = 9.9 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
155535667 178838 0 None 562 2 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4472007 178838 0 None 562 2 Human 9.8 pEC50 = 9.8 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476369 176970 0 None 3388 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4444891 176970 0 None 3388 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476336 177990 0 None 630 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4459424 177990 0 None 630 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476365 180629 0 None 794 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4539100 180629 0 None 794 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
2181 8113 42 None -6 4 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00132
2182 8113 42 None -6 4 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00132
27991 8113 42 None -6 4 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00132
5311065 8113 42 None -6 4 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00132
CHEMBL1429 8113 42 None -6 4 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00132
CHEMBL264448 8113 42 None -6 4 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00132
DB00035 8113 42 None -6 4 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.9b00132
132095331 182003 0 None 645 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4571464 182003 0 None 645 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476362 177727 0 None 575 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4455496 177727 0 None 575 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476356 178988 0 None 1513 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4473843 178988 0 None 1513 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476335 177096 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4446853 177096 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476329 179945 0 None 954 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4521807 179945 0 None 954 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476347 182114 0 None 501 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4574065 182114 0 None 501 2 Human 9.7 pEC50 = 9.7 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476358 177447 0 None 2089 2 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4451555 177447 0 None 2089 2 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476331 180305 0 None 2089 2 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4531173 180305 0 None 2089 2 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476355 180643 3 None -5 3 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4539370 180643 3 None -5 3 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476366 180832 0 None 741 2 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4543908 180832 0 None 741 2 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476346 181294 0 None 588 2 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4555263 181294 0 None 588 2 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476341 177461 0 None 1288 2 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4451692 177461 0 None 1288 2 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476385 181390 0 None 169 2 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4557473 181390 0 None 169 2 Human 9.6 pEC50 = 9.6 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476359 178188 0 None 524 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4462616 178188 0 None 524 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
90468623 180941 0 None 588 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4546884 180941 0 None 588 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476342 181373 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4557118 181373 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
155513872 176577 0 None 331 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4439313 176577 0 None 331 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476383 176537 0 None 457 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4438723 176537 0 None 457 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476348 180301 0 None 457 3 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4531053 180301 0 None 457 3 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476344 180157 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4527761 180157 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476367 176980 0 None 758 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4445168 176980 0 None 758 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476332 176321 0 None 630 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4435502 176321 0 None 630 2 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
155542670 179939 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4521602 179939 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
118476339 179576 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4513567 179576 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
90469676 181184 0 None 2089 2 Human 9.4 pEC50 = 9.4 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4552500 181184 0 None 2089 2 Human 9.4 pEC50 = 9.4 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL1819440 215792 23 None -1 5 Human 9.4 pEC50 = 9.4 Functional
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
ChEMBL 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 10.1021/jm200278m
118476333 176390 0 None 1288 2 Human 9.4 pEC50 = 9.4 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL4436571 176390 0 None 1288 2 Human 9.4 pEC50 = 9.4 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.9b00132
CHEMBL1819440 215792 23 None -1 5 Human 9.4 pEC50 = 9.4 Functional
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
ChEMBL 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 10.1021/jm200278m
3537 10776 22 None 3 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at V2 receptor (unknown origin) by cAMP accumulation assayAgonist activity at V2 receptor (unknown origin) by cAMP accumulation assay
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/acs.jmedchem.8b00697
5311500 10776 22 None 3 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at V2 receptor (unknown origin) by cAMP accumulation assayAgonist activity at V2 receptor (unknown origin) by cAMP accumulation assay
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/acs.jmedchem.8b00697
CHEMBL363910 10776 22 None 3 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at V2 receptor (unknown origin) by cAMP accumulation assayAgonist activity at V2 receptor (unknown origin) by cAMP accumulation assay
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/acs.jmedchem.8b00697
3537 10776 22 None 3 4 Human 9.1 pEC50 = 9.1 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1016/j.bmcl.2005.10.107
5311500 10776 22 None 3 4 Human 9.1 pEC50 = 9.1 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1016/j.bmcl.2005.10.107
CHEMBL363910 10776 22 None 3 4 Human 9.1 pEC50 = 9.1 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1016/j.bmcl.2005.10.107
44520851 206578 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
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
ChEMBL 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 10.1016/j.bmc.2009.10.038
CHEMBL594026 206578 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
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
ChEMBL 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 10.1016/j.bmc.2009.10.038
44520849 208492 0 None - 1 Human 9.0 pEC50 = 9 Functional
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
ChEMBL 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 10.1016/j.bmc.2009.10.038
CHEMBL606464 208492 0 None - 1 Human 9.0 pEC50 = 9 Functional
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
ChEMBL 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 10.1016/j.bmc.2009.10.038
44520852 206487 0 None - 1 Human 9.0 pEC50 = 9 Functional
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
ChEMBL 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 10.1016/j.bmc.2009.10.038
CHEMBL593325 206487 0 None - 1 Human 9.0 pEC50 = 9 Functional
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
ChEMBL 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 10.1016/j.bmc.2009.10.038
44520850 206643 0 None - 1 Human 9.0 pEC50 = 9 Functional
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
ChEMBL 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 10.1016/j.bmc.2009.10.038
CHEMBL594488 206643 0 None - 1 Human 9.0 pEC50 = 9 Functional
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
ChEMBL 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 10.1016/j.bmc.2009.10.038
44520880 19349 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 550 5 1 4 6.0 CC1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2008.09.039
CHEMBL1186825 19349 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 550 5 1 4 6.0 CC1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2008.09.039
CHEMBL479918 19349 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 550 5 1 4 6.0 CC1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2008.09.039
CHEMBL1819441 215793 0 None -18 4 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819441 215793 0 None -18 4 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 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 10.1021/jm200278m
9824954 80635 0 None 43 3 Human 8.8 pEC50 = 8.8 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL 449 2 1 5 5.5 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2005.10.107
CHEMBL201889 80635 0 None 43 3 Human 8.8 pEC50 = 8.8 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL 449 2 1 5 5.5 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2005.10.107
9959174 201266 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL487164 201266 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL528996 201266 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
9959174 201266 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
CHEMBL487164 201266 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
CHEMBL528996 201266 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
10281429 195132 0 None - 1 Human 8.0 pEC50 = 8 Functional
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
ChEMBL 568 7 1 4 4.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1C[C@H](OCc2ccccc2)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL501078 195132 0 None - 1 Human 8.0 pEC50 = 8 Functional
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
ChEMBL 568 7 1 4 4.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1C[C@H](OCc2ccccc2)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
25181105 195697 0 None - 1 Human 8.0 pEC50 = 8 Functional
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
ChEMBL 463 5 2 2 5.8 CCc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL507816 195697 0 None - 1 Human 8.0 pEC50 = 8 Functional
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
ChEMBL 463 5 2 2 5.8 CCc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
25178785 183522 0 None - 1 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 449 4 1 4 3.8 COC(=O)[C@@H]1CCCN1C(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C 10.1021/jm8008162
CHEMBL460303 183522 0 None - 1 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 449 4 1 4 3.8 COC(=O)[C@@H]1CCCN1C(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C 10.1021/jm8008162
18759824 196622 0 None - 1 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 448 5 2 3 3.4 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N1CCCC1 10.1021/jm8008162
CHEMBL516629 196622 0 None - 1 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 448 5 2 3 3.4 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N1CCCC1 10.1021/jm8008162
25180885 187119 0 None - 1 Human 6.0 pEC50 = 6 Functional
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
ChEMBL 464 4 1 4 3.2 Cc1cc(C(=O)N2CCCOc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL475129 187119 0 None - 1 Human 6.0 pEC50 = 6 Functional
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
ChEMBL 464 4 1 4 3.2 Cc1cc(C(=O)N2CCCOc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
44520882 19353 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 550 5 1 4 6.1 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1186831 19353 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 550 5 1 4 6.1 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL480104 19353 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 550 5 1 4 6.1 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
145963213 168260 0 None -309 4 Human 5.0 pEC50 = 5.0 Functional
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
ChEMBL 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 10.1016/j.bmc.2018.03.019
CHEMBL4127791 168260 0 None -309 4 Human 5.0 pEC50 = 5.0 Functional
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
ChEMBL 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 10.1016/j.bmc.2018.03.019
25178587 181369 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 465 5 2 3 5.3 COc1cc(CNC(=O)Nc2c(F)cccc2F)ccc1C(=O)N1CCCCc2ccccc21 10.1021/jm8008162
CHEMBL455696 181369 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 465 5 2 3 5.3 COc1cc(CNC(=O)Nc2c(F)cccc2F)ccc1C(=O)N1CCCCc2ccccc21 10.1021/jm8008162
11169 7584 37 None -173 5 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.8b00697
131676677 7584 37 None -173 5 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.8b00697
165708555 7584 37 None -173 5 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.8b00697
16681432 7584 37 None -173 5 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.8b00697
495 7584 37 None -173 5 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.8b00697
CHEMBL3301668 7584 37 None -173 5 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.8b00697
DB01282 7584 37 None -173 5 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.8b00697
44520881 19350 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 550 5 1 4 6.1 CC1CCCN1c1ccc(C(=O)N2CCC(F)(F)/C(=C\C(=O)NCc3ccccn3)c3ccccc32)c(Cl)c1 10.1016/j.bmc.2008.09.039
CHEMBL1186826 19350 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 550 5 1 4 6.1 CC1CCCN1c1ccc(C(=O)N2CCC(F)(F)/C(=C\C(=O)NCc3ccccn3)c3ccccc32)c(Cl)c1 10.1016/j.bmc.2008.09.039
CHEMBL479919 19350 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 550 5 1 4 6.1 CC1CCCN1c1ccc(C(=O)N2CCC(F)(F)/C(=C\C(=O)NCc3ccccn3)c3ccccc32)c(Cl)c1 10.1016/j.bmc.2008.09.039
CHEMBL1817671 215761 0 None -61 3 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817671 215761 0 None -61 3 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819548 215802 0 None -218 4 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819554 215807 0 None -1513 4 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 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 10.1021/jm200278m
25178963 187290 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 499 4 1 4 3.8 Cc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL475333 187290 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 499 4 1 4 3.8 Cc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
18759822 197564 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 451 5 2 4 4.1 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)OC(C)(C)C 10.1021/jm8008162
CHEMBL518349 197564 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 451 5 2 4 4.1 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)OC(C)(C)C 10.1021/jm8008162
CHEMBL1819548 215802 0 None -218 4 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 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 10.1021/jm200278m
53362156 71394 0 None -17 3 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817690 71394 0 None -17 3 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819553 215806 0 None -93 3 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819554 215807 0 None -1513 4 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 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 10.1021/jm200278m
53362156 71394 0 None -17 3 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817690 71394 0 None -17 3 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819553 215806 0 None -93 3 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 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 10.1021/jm200278m
10456892 72839 0 None -74 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
ChEMBL 458 3 0 7 3.0 CS(=O)(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
CHEMBL1837041 72839 0 None -74 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
ChEMBL 458 3 0 7 3.0 CS(=O)(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
44563579 181370 0 None -6 2 Rat 7.9 pEC50 = 7.9 Functional
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
ChEMBL 449 4 2 2 5.6 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL455699 181370 0 None -6 2 Rat 7.9 pEC50 = 7.9 Functional
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
ChEMBL 449 4 2 2 5.6 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
25178591 180194 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 413 4 2 2 5.3 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1ccccc1 10.1021/jm8008162
CHEMBL452853 180194 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 413 4 2 2 5.3 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1ccccc1 10.1021/jm8008162
CHEMBL1817705 215766 0 None -512 5 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817705 215766 0 None -512 5 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817706 215767 0 None -1348 5 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 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 10.1021/jm200278m
21083206 181023 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 430 4 3 3 4.0 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1ccc[nH]c1=O 10.1021/jm8008162
CHEMBL454894 181023 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 430 4 3 3 4.0 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1ccc[nH]c1=O 10.1021/jm8008162
15896091 183531 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 423 6 2 4 3.3 CCOC(=O)CNC(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C 10.1021/jm8008162
CHEMBL460319 183531 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 423 6 2 4 3.3 CCOC(=O)CNC(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C 10.1021/jm8008162
18759812 183532 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 437 6 2 4 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)OC(C)C 10.1021/jm8008162
CHEMBL460320 183532 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 437 6 2 4 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)OC(C)C 10.1021/jm8008162
25180887 200003 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 499 4 1 4 3.8 Cc1cc(C(=O)N2CCc3cccn3-c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL523596 200003 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 499 4 1 4 3.8 Cc1cc(C(=O)N2CCc3cccn3-c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL1817706 215767 0 None -1348 5 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 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 10.1021/jm200278m
25180697 186009 0 None -3 2 Rat 7.8 pEC50 = 7.8 Functional
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
ChEMBL 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 10.1021/jm8008162
CHEMBL472697 186009 0 None -3 2 Rat 7.8 pEC50 = 7.8 Functional
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
ChEMBL 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 10.1021/jm8008162
18759808 183681 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 462 5 2 3 3.8 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N1CCCCC1 10.1021/jm8008162
CHEMBL461725 183681 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 462 5 2 3 3.8 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N1CCCCC1 10.1021/jm8008162
10298385 197367 33 None -6 2 Rat 6.8 pEC50 = 6.8 Functional
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
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL518043 197367 33 None -6 2 Rat 6.8 pEC50 = 6.8 Functional
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
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL1819542 215796 9 None -1258 4 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819542 215796 9 None -1258 4 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 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 10.1021/jm200278m
44520861 187598 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 548 5 1 6 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccnn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL475684 187598 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 548 5 1 6 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccnn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
53362548 71407 0 None -602 4 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817751 71407 0 None -602 4 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817702 215763 0 None -4786 4 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 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 10.1021/jm200278m
53362548 71407 0 None -602 4 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817751 71407 0 None -602 4 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 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 10.1021/jm200278m
53362202 71395 0 None -13 3 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817691 71395 0 None -13 3 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817702 215763 0 None -4786 4 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 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 10.1021/jm200278m
53362155 71577 0 None -1513 3 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819560 71577 0 None -1513 3 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 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 10.1021/jm200278m
53362202 71395 0 None -13 3 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817691 71395 0 None -13 3 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 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 10.1021/jm200278m
25178962 187118 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 498 4 1 3 4.3 Cc1cc(C(=O)N2CCCC(F)(F)c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL475128 187118 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 498 4 1 3 4.3 Cc1cc(C(=O)N2CCCC(F)(F)c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
53362155 71577 0 None -1513 3 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819560 71577 0 None -1513 3 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 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 10.1021/jm200278m
21083210 181368 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 453 4 2 2 5.4 O=C(NCc1ccc(C(=O)N2CCCCc3ccccc32)c(F)c1)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL455695 181368 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 453 4 2 2 5.4 O=C(NCc1ccc(C(=O)N2CCCCc3ccccc32)c(F)c1)Nc1c(F)cccc1F 10.1021/jm8008162
15896092 183530 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 395 5 3 3 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)O 10.1021/jm8008162
CHEMBL460318 183530 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 395 5 3 3 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)O 10.1021/jm8008162
CHEMBL1817708 215769 0 None -234 4 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 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 10.1021/jm200278m
2173 9730 13 None -1 2 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/acs.jmedchem.8b00697
3038506 9730 13 None -1 2 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/acs.jmedchem.8b00697
CHEMBL332447 9730 13 None -1 2 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/acs.jmedchem.8b00697
DB05838 9730 13 None -1 2 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/acs.jmedchem.8b00697
145961670 168143 0 None -1348 4 Human 4.7 pEC50 = 4.7 Functional
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
ChEMBL 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 10.1016/j.bmc.2018.03.019
CHEMBL4126100 168143 0 None -1348 4 Human 4.7 pEC50 = 4.7 Functional
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
ChEMBL 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 10.1016/j.bmc.2018.03.019
CHEMBL1817708 215769 0 None -234 4 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 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 10.1021/jm200278m
44563579 181370 0 None 6 2 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 449 4 2 2 5.6 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL455699 181370 0 None 6 2 Human 8.7 pEC50 = 8.7 Functional
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
ChEMBL 449 4 2 2 5.6 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
10162731 183769 0 None 17 2 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 478 4 2 4 2.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1C[C@H](O)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL462574 183769 0 None 17 2 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 478 4 2 4 2.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1C[C@H](O)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
44520848 206723 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 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 10.1016/j.bmc.2009.10.038
CHEMBL594953 206723 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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
ChEMBL 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 10.1016/j.bmc.2009.10.038
44563371 185716 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 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 10.1021/jm8008162
CHEMBL470326 185716 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 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 10.1021/jm8008162
CHEMBL1819549 215803 0 None -323 4 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819549 215803 0 None -323 4 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 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 10.1021/jm200278m
53363016 71574 0 None -34 4 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819557 71574 0 None -34 4 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 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 10.1021/jm200278m
2042 9757 58 None -26 5 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.8b00697
2174 9757 58 None -26 5 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.8b00697
2176 9757 58 None -26 5 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.8b00697
439302 9757 58 None -26 5 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.8b00697
CHEMBL395429 9757 58 None -26 5 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.8b00697
DB00107 9757 58 None -26 5 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.8b00697
18759802 183754 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 394 5 3 3 2.3 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(N)=O 10.1021/jm8008162
CHEMBL462409 183754 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 394 5 3 3 2.3 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(N)=O 10.1021/jm8008162
53363016 71574 0 None -34 4 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819557 71574 0 None -34 4 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 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 10.1021/jm200278m
10345610 72838 0 None -204 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
ChEMBL 422 2 0 6 3.6 CC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
CHEMBL1837040 72838 0 None -204 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
ChEMBL 422 2 0 6 3.6 CC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
25180884 186288 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 476 4 1 3 4.3 Cc1cc(C(=O)N2CCCC(C)c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL474120 186288 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 476 4 1 3 4.3 Cc1cc(C(=O)N2CCCC(C)c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
25178961 186286 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 478 4 2 4 3.2 Cc1cc(C(=O)N2CCCC(O)c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL474119 186286 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 478 4 2 4 3.2 Cc1cc(C(=O)N2CCCC(O)c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
135506374 144678 23 None -48 4 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 581 5 4 8 4.1 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCN(Cc2cc(O)cc(O)c2)CC1 10.1021/acs.jmedchem.8b00697
CHEMBL3763342 144678 23 None -48 4 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 581 5 4 8 4.1 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCN(Cc2cc(O)cc(O)c2)CC1 10.1021/acs.jmedchem.8b00697
10298385 197367 33 None 6 2 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL518043 197367 33 None 6 2 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL1819547 215801 0 None -131 4 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819547 215801 0 None -131 4 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817707 215768 0 None -1621 5 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817707 215768 0 None -1621 5 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 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 10.1021/jm200278m
53362259 71399 0 None -645 3 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817696 71399 0 None -645 3 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 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 10.1021/jm200278m
53363017 71575 0 None -67 3 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819558 71575 0 None -67 3 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 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 10.1021/jm200278m
11454 10350 11 None -4786 5 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL None None None None 10.1021/jm200278m
53330936 10350 11 None -4786 5 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL None None None None 10.1021/jm200278m
CHEMBL1817709 10350 11 None -4786 5 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL None None None None 10.1021/jm200278m
DB12495 10350 11 None -4786 5 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL None None None None 10.1021/jm200278m
53362259 71399 0 None -645 3 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817696 71399 0 None -645 3 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 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 10.1021/jm200278m
53363017 71575 0 None -67 3 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819558 71575 0 None -67 3 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 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 10.1021/jm200278m
11237434 72834 10 None -102 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
ChEMBL 394 2 0 6 3.6 CN1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
CHEMBL1837037 72834 10 None -102 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
ChEMBL 394 2 0 6 3.6 CN1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
25178960 186036 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 476 4 1 4 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CC(=O)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL472900 186036 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 476 4 1 4 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CC(=O)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
25178784 183525 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 484 7 3 3 4.1 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)NCc1ccccc1 10.1021/jm8008162
CHEMBL460308 183525 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 484 7 3 3 4.1 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)NCc1ccccc1 10.1021/jm8008162
11454 10350 11 None -4786 5 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL None None None None 10.1021/jm200278m
53330936 10350 11 None -4786 5 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL None None None None 10.1021/jm200278m
CHEMBL1817709 10350 11 None -4786 5 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL None None None None 10.1021/jm200278m
DB12495 10350 11 None -4786 5 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL None None None None 10.1021/jm200278m
CHEMBL1817704 215765 0 None -2238 5 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 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 10.1021/jm200278m
2042 9757 58 None -26 5 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL None None None None 10.1016/j.bmc.2018.03.019
2174 9757 58 None -26 5 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL None None None None 10.1016/j.bmc.2018.03.019
2176 9757 58 None -26 5 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL None None None None 10.1016/j.bmc.2018.03.019
439302 9757 58 None -26 5 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL None None None None 10.1016/j.bmc.2018.03.019
CHEMBL395429 9757 58 None -26 5 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL None None None None 10.1016/j.bmc.2018.03.019
DB00107 9757 58 None -26 5 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL None None None None 10.1016/j.bmc.2018.03.019
CHEMBL1817704 215765 0 None -2238 5 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 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 10.1021/jm200278m
44520879 19506 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 536 5 1 4 5.7 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1187728 19506 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 536 5 1 4 5.7 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL516757 19506 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 536 5 1 4 5.7 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
25180696 183727 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 478 4 1 3 4.5 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/jm8008162
CHEMBL462212 183727 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 478 4 1 3 4.5 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/jm8008162
25180311 181374 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 431 4 2 2 5.4 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1ccccc1F 10.1021/jm8008162
CHEMBL455717 181374 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 431 4 2 2 5.4 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1ccccc1F 10.1021/jm8008162
53362154 71576 0 None -144 3 Human 5.5 pEC50 = 5.5 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819559 71576 0 None -144 3 Human 5.5 pEC50 = 5.5 Functional
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
ChEMBL 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 10.1021/jm200278m
53362154 71576 0 None -144 3 Human 5.5 pEC50 = 5.5 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819559 71576 0 None -144 3 Human 5.5 pEC50 = 5.5 Functional
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
ChEMBL 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 10.1021/jm200278m
56672570 72835 0 None -9 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
ChEMBL 438 2 0 7 3.8 COC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
CHEMBL1837038 72835 0 None -9 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
ChEMBL 438 2 0 7 3.8 COC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
CHEMBL1819550 215804 0 None -151 4 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819550 215804 0 None -151 4 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 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 10.1021/jm200278m
25180695 183650 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 490 6 1 3 4.5 CCN(CC)C(=O)[C@@H]1CCCN1C(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C 10.1021/jm8008162
CHEMBL461519 183650 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 490 6 1 3 4.5 CCN(CC)C(=O)[C@@H]1CCCN1C(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C 10.1021/jm8008162
145960494 168340 0 None -33 4 Human 5.4 pEC50 = 5.4 Functional
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
ChEMBL 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 10.1016/j.bmc.2018.03.019
CHEMBL4128839 168340 0 None -33 4 Human 5.4 pEC50 = 5.4 Functional
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
ChEMBL 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 10.1016/j.bmc.2018.03.019
15896094 196640 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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
ChEMBL 409 5 2 4 3.0 COC(=O)CNC(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C 10.1021/jm8008162
CHEMBL516788 196640 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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
ChEMBL 409 5 2 4 3.0 COC(=O)CNC(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C 10.1021/jm8008162
CHEMBL1817752 215771 0 None -2691 4 Human 5.4 pEC50 = 5.4 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817752 215771 0 None -2691 4 Human 5.4 pEC50 = 5.4 Functional
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
ChEMBL 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 10.1021/jm200278m
25178787 183651 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL461520 183651 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL1819556 215809 0 None -407 4 Human 6.4 pEC50 = 6.4 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819556 215809 0 None -407 4 Human 6.4 pEC50 = 6.4 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817761 215780 0 None -1202 5 Human 6.4 pEC50 = 6.4 Functional
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
ChEMBL 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 10.1021/jm200278m
25178786 183775 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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
ChEMBL 491 4 1 4 5.0 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)OC(C)(C)C 10.1021/jm8008162
CHEMBL462595 183775 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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
ChEMBL 491 4 1 4 5.0 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)OC(C)(C)C 10.1021/jm8008162
CHEMBL1817761 215780 0 None -1202 5 Human 6.4 pEC50 = 6.4 Functional
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
ChEMBL 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 10.1021/jm200278m
145962220 168356 0 None -114 4 Human 5.4 pEC50 = 5.4 Functional
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
ChEMBL 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 10.1016/j.bmc.2018.03.019
CHEMBL4129142 168356 0 None -114 4 Human 5.4 pEC50 = 5.4 Functional
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
ChEMBL 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 10.1016/j.bmc.2018.03.019
145976595 170494 0 None 2 3 Human 8.4 pEC50 = 8.4 Functional
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
ChEMBL 408 2 1 4 4.9 Cc1ccn(C(=O)Nc2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL4205046 170494 0 None 2 3 Human 8.4 pEC50 = 8.4 Functional
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
ChEMBL 408 2 1 4 4.9 Cc1ccn(C(=O)Nc2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL1819541 215795 0 None -17 4 Human 8.4 pEC50 = 8.4 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819541 215795 0 None -17 4 Human 8.4 pEC50 = 8.4 Functional
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
ChEMBL 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 10.1021/jm200278m
42629368 189444 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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
ChEMBL 457 3 1 4 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL478902 189444 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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
ChEMBL 457 3 1 4 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
25180697 186009 0 None 3 2 Human 8.4 pEC50 = 8.4 Functional
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
ChEMBL 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 10.1021/jm8008162
CHEMBL472697 186009 0 None 3 2 Human 8.4 pEC50 = 8.4 Functional
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
ChEMBL 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 10.1021/jm8008162
10206789 196496 0 None 13 2 Human 8.3 pEC50 = 8.3 Functional
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
ChEMBL 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 10.1021/jm8008162
CHEMBL515607 196496 0 None 13 2 Human 8.3 pEC50 = 8.3 Functional
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
ChEMBL 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 10.1021/jm8008162
25181104 195863 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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
ChEMBL 469 4 2 2 5.9 O=C(NCc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL509960 195863 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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
ChEMBL 469 4 2 2 5.9 O=C(NCc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1)Nc1c(F)cccc1F 10.1021/jm8008162
10444 9106 14 None -9 4 Human 7.4 pEC50 = 7.4 Functional
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
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
139030525 9106 14 None -9 4 Human 7.4 pEC50 = 7.4 Functional
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
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
145711714 9106 14 None -9 4 Human 7.4 pEC50 = 7.4 Functional
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
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
CHEMBL4204210 9106 14 None -9 4 Human 7.4 pEC50 = 7.4 Functional
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
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
10162731 183769 0 None -17 2 Rat 7.4 pEC50 = 7.4 Functional
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
ChEMBL 478 4 2 4 2.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1C[C@H](O)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL462574 183769 0 None -17 2 Rat 7.4 pEC50 = 7.4 Functional
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
ChEMBL 478 4 2 4 2.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1C[C@H](O)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
25178959 196097 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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
ChEMBL 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 10.1021/jm8008162
CHEMBL512349 196097 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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
ChEMBL 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 10.1021/jm8008162
CHEMBL1819552 215805 0 None -42 3 Human 6.3 pEC50 = 6.3 Functional
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
ChEMBL 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 10.1021/jm200278m
9954641 181375 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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
ChEMBL 435 4 2 2 5.3 O=C(NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL455718 181375 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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
ChEMBL 435 4 2 2 5.3 O=C(NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL1819552 215805 0 None -42 3 Human 6.3 pEC50 = 6.3 Functional
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
ChEMBL 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 10.1021/jm200278m
44563370 186162 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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
ChEMBL 512 5 1 3 4.2 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CC(C(F)F)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL473917 186162 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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
ChEMBL 512 5 1 3 4.2 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CC(C(F)F)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
6918573 72051 3 None 1 2 Rat 7.3 pEC50 = 7.3 Functional
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
ChEMBL 422 5 2 3 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N(C)C 10.1021/jm8008162
CHEMBL182852 72051 3 None 1 2 Rat 7.3 pEC50 = 7.3 Functional
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
ChEMBL 422 5 2 3 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N(C)C 10.1021/jm8008162
53362547 71406 0 None -1348 3 Human 5.3 pEC50 = 5.3 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817750 71406 0 None -1348 3 Human 5.3 pEC50 = 5.3 Functional
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
ChEMBL 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 10.1021/jm200278m
53362547 71406 0 None -1348 3 Human 5.3 pEC50 = 5.3 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817750 71406 0 None -1348 3 Human 5.3 pEC50 = 5.3 Functional
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
ChEMBL 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 10.1021/jm200278m
6918573 72051 3 None -1 2 Human 7.2 pEC50 = 7.2 Functional
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
ChEMBL 422 5 2 3 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N(C)C 10.1021/jm8008162
CHEMBL182852 72051 3 None -1 2 Human 7.2 pEC50 = 7.2 Functional
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
ChEMBL 422 5 2 3 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N(C)C 10.1021/jm8008162
42629369 188973 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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
ChEMBL 500 5 2 5 4.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL478283 188973 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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
ChEMBL 500 5 2 5 4.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
42629369 188973 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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
ChEMBL 500 5 2 5 4.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.10.038
CHEMBL478283 188973 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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
ChEMBL 500 5 2 5 4.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.10.038
44520872 19382 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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
ChEMBL 533 5 1 5 5.3 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3cccn3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1186989 19382 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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
ChEMBL 533 5 1 5 5.3 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3cccn3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL485760 19382 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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
ChEMBL 533 5 1 5 5.3 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3cccn3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
44520883 19467 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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
ChEMBL 564 5 1 4 6.5 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1187505 19467 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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
ChEMBL 564 5 1 4 6.5 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL505517 19467 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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
ChEMBL 564 5 1 4 6.5 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
10206789 196496 0 None -13 2 Rat 7.2 pEC50 = 7.2 Functional
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
ChEMBL 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 10.1021/jm8008162
CHEMBL515607 196496 0 None -13 2 Rat 7.2 pEC50 = 7.2 Functional
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
ChEMBL 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 10.1021/jm8008162
10444 9106 14 None -9 4 Human 6.2 pEC50 = 6.2 Functional
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
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
139030525 9106 14 None -9 4 Human 6.2 pEC50 = 6.2 Functional
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
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
145711714 9106 14 None -9 4 Human 6.2 pEC50 = 6.2 Functional
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
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
CHEMBL4204210 9106 14 None -9 4 Human 6.2 pEC50 = 6.2 Functional
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
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
11169 7584 37 None -173 5 Human 5.2 pEC50 = 5.2 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.8b00697
131676677 7584 37 None -173 5 Human 5.2 pEC50 = 5.2 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.8b00697
165708555 7584 37 None -173 5 Human 5.2 pEC50 = 5.2 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.8b00697
16681432 7584 37 None -173 5 Human 5.2 pEC50 = 5.2 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.8b00697
495 7584 37 None -173 5 Human 5.2 pEC50 = 5.2 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.8b00697
CHEMBL3301668 7584 37 None -173 5 Human 5.2 pEC50 = 5.2 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.8b00697
DB01282 7584 37 None -173 5 Human 5.2 pEC50 = 5.2 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.8b00697
25180508 183773 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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
ChEMBL 435 4 2 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)O 10.1021/jm8008162
CHEMBL462590 183773 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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
ChEMBL 435 4 2 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)O 10.1021/jm8008162
CHEMBL1819543 215797 0 None -144 4 Human 7.1 pEC50 = 7.1 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817703 215764 0 None -24 3 Human 6.1 pEC50 = 6.1 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817703 215764 0 None -24 3 Human 6.1 pEC50 = 6.1 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819543 215797 0 None -144 4 Human 7.1 pEC50 = 7.1 Functional
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
ChEMBL 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 10.1021/jm200278m
25180507 196691 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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
ChEMBL 485 7 2 4 4.5 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)OCc1ccccc1 10.1021/jm8008162
CHEMBL516985 196691 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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
ChEMBL 485 7 2 4 4.5 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)OCc1ccccc1 10.1021/jm8008162
CHEMBL1819555 215808 0 None -3019 4 Human 6.1 pEC50 = 6.1 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819555 215808 0 None -3019 4 Human 6.1 pEC50 = 6.1 Functional
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
ChEMBL 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 10.1021/jm200278m
2042 9757 58 None -26 5 Human 6.1 pEC50 = 6.1 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.8b00697
2174 9757 58 None -26 5 Human 6.1 pEC50 = 6.1 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.8b00697
2176 9757 58 None -26 5 Human 6.1 pEC50 = 6.1 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.8b00697
439302 9757 58 None -26 5 Human 6.1 pEC50 = 6.1 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.8b00697
CHEMBL395429 9757 58 None -26 5 Human 6.1 pEC50 = 6.1 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.8b00697
DB00107 9757 58 None -26 5 Human 6.1 pEC50 = 6.1 Functional
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
ChEMBL None None None None 10.1021/acs.jmedchem.8b00697
21083212 181020 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
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
ChEMBL 463 4 2 2 5.9 Cc1cc(C(=O)N2CCCCc3ccccc32)cc(C)c1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL454892 181020 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
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
ChEMBL 463 4 2 2 5.9 Cc1cc(C(=O)N2CCCCc3ccccc32)cc(C)c1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
25178592 183753 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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
ChEMBL 471 6 2 4 4.4 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)Oc1ccccc1 10.1021/jm8008162
CHEMBL462408 183753 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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
ChEMBL 471 6 2 4 4.4 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)Oc1ccccc1 10.1021/jm8008162
25180886 187643 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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
ChEMBL 510 4 1 3 4.6 Cc1cc(C(=O)N2CCc3ccccc3-c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL475733 187643 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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
ChEMBL 510 4 1 3 4.6 Cc1cc(C(=O)N2CCc3ccccc3-c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
135413563 129708 25 None -107 3 Human 6.1 pEC50 = 6.1 Functional
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
ChEMBL 600 4 2 7 4.3 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1021/acs.jmedchem.8b00697
CHEMBL360648 129708 25 None -107 3 Human 6.1 pEC50 = 6.1 Functional
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
ChEMBL 600 4 2 7 4.3 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1021/acs.jmedchem.8b00697
CHEMBL1819540 215794 0 None -64 3 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1819540 215794 0 None -64 3 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 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 10.1021/jm200278m
25180509 196620 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 477 5 1 4 4.6 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)OC(C)C 10.1021/jm8008162
CHEMBL516627 196620 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 477 5 1 4 4.6 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)OC(C)C 10.1021/jm8008162
CHEMBL1817756 215775 0 None -1548 5 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817756 215775 0 None -1548 5 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817770 215789 0 None -691 4 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 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 10.1021/jm200278m
CHEMBL1817770 215789 0 None -691 4 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 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 10.1021/jm200278m
10411308 208013 0 None 2 3 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at V2 receptor (unknown origin)Antagonist activity at V2 receptor (unknown origin)
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.8b00697
CHEMBL603708 208013 0 None 2 3 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at V2 receptor (unknown origin)Antagonist activity at V2 receptor (unknown origin)
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.8b00697
44357890 175172 0 None 39 3 Human 9.0 pIC50 = 9.0 Functional
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%
ChEMBL 462 5 1 3 6.0 Cc1ccccc1OCC(=O)Nc1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(C)c1 10.1021/jm000108p
CHEMBL434654 175172 0 None 39 3 Human 9.0 pIC50 = 9.0 Functional
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%
ChEMBL 462 5 1 3 6.0 Cc1ccccc1OCC(=O)Nc1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(C)c1 10.1021/jm000108p
11432362 100912 0 None -1 2 Human 7.0 pIC50 = 7 Functional
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
ChEMBL 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 10.1016/j.bmcl.2007.09.059
CHEMBL249340 100912 0 None -1 2 Human 7.0 pIC50 = 7 Functional
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
ChEMBL 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 10.1016/j.bmcl.2007.09.059
10461417 114078 0 None -7 2 Human 7.0 pIC50 = 7 Functional
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
ChEMBL 612 8 2 4 6.6 CN(C)CCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL317243 114078 0 None -7 2 Human 7.0 pIC50 = 7 Functional
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
ChEMBL 612 8 2 4 6.6 CN(C)CCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
44352783 123559 0 None 4 2 Human 7.0 pIC50 = 7 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 508 6 2 4 6.5 O=C(Nc1ccc(C(=O)N2CCC(CCO)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
CHEMBL337725 123559 0 None 4 2 Human 7.0 pIC50 = 7 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 508 6 2 4 6.5 O=C(Nc1ccc(C(=O)N2CCC(CCO)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
44336404 117736 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
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
ChEMBL 568 7 2 4 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN(C)C)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL326225 117736 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
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
ChEMBL 568 7 2 4 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN(C)C)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
25132999 161682 0 None -3 2 Human 6.0 pIC50 = 6.0 Functional
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
ChEMBL 572 5 2 5 6.0 COc1cc(C(=O)N2CC[C@]3(C=C(C4=NCCN4)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL400860 161682 0 None -3 2 Human 6.0 pIC50 = 6.0 Functional
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
ChEMBL 572 5 2 5 6.0 COc1cc(C(=O)N2CC[C@]3(C=C(C4=NCCN4)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
151171 7947 50 None -3 2 Human 8.0 pIC50 = 8.0 Functional
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
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
216322 7947 50 None -3 2 Human 8.0 pIC50 = 8.0 Functional
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
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
2203 7947 50 None -3 2 Human 8.0 pIC50 = 8.0 Functional
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
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
732 7947 50 None -3 2 Human 8.0 pIC50 = 8.0 Functional
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
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
CHEMBL1755 7947 50 None -3 2 Human 8.0 pIC50 = 8.0 Functional
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
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
DB00872 7947 50 None -3 2 Human 8.0 pIC50 = 8.0 Functional
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
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
25133000 100969 0 None 2 2 Human 8.0 pIC50 = 8.0 Functional
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
ChEMBL 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 10.1016/j.bmcl.2007.09.059
CHEMBL249740 100969 0 None 2 2 Human 8.0 pIC50 = 8.0 Functional
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
ChEMBL 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 10.1016/j.bmcl.2007.09.059
216237 10615 89 None 41 7 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 minsAntagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
2226 10615 89 None 41 7 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 minsAntagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
4110 10615 89 None 41 7 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 minsAntagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
443894 10615 89 None 41 7 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 minsAntagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
CHEMBL344159 10615 89 None 41 7 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 minsAntagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
DB06212 10615 89 None 41 7 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 minsAntagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
11261339 161399 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
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
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CCC3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL399289 161399 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
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
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CCC3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
145976595 170494 0 None 2 3 Human 7.9 pIC50 = 7.9 Functional
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
ChEMBL 408 2 1 4 4.9 Cc1ccn(C(=O)Nc2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL4205046 170494 0 None 2 3 Human 7.9 pIC50 = 7.9 Functional
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
ChEMBL 408 2 1 4 4.9 Cc1ccn(C(=O)Nc2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
23598597 100872 0 None 91 2 Human 6.9 pIC50 = 6.9 Functional
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
ChEMBL 528 5 2 4 5.8 COc1cc(NC(=O)c2cc(F)ccc2C)ccc1C(=O)N1CCC2(C=C(C(=O)O)CC2)Cc2ccccc21 10.1016/j.bmcl.2007.09.059
CHEMBL249133 100872 0 None 91 2 Human 6.9 pIC50 = 6.9 Functional
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
ChEMBL 528 5 2 4 5.8 COc1cc(NC(=O)c2cc(F)ccc2C)ccc1C(=O)N1CCC2(C=C(C(=O)O)CC2)Cc2ccccc21 10.1016/j.bmcl.2007.09.059
11238362 175687 0 None -5 2 Human 6.8 pIC50 = 6.8 Functional
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
ChEMBL 562 6 2 4 6.5 CCOc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL438523 175687 0 None -5 2 Human 6.8 pIC50 = 6.8 Functional
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
ChEMBL 562 6 2 4 6.5 CCOc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
11683187 206711 44 None -20 2 Human 5.8 pIC50 = 5.8 Functional
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
ChEMBL 419 7 0 8 2.9 COCc1nnc(N2CC(Oc3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acs.jmedchem.8b00697
CHEMBL594828 206711 44 None -20 2 Human 5.8 pIC50 = 5.8 Functional
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
ChEMBL 419 7 0 8 2.9 COCc1nnc(N2CC(Oc3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acs.jmedchem.8b00697
168289573 198618 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 minsAntagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
ChEMBL 572 8 2 4 7.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCCCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5198918 198618 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 minsAntagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
ChEMBL 572 8 2 4 7.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCCCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
44336636 170944 0 None -7 2 Human 6.8 pIC50 = 6.8 Functional
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
ChEMBL 585 7 3 4 6.0 O=C(NCCO)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL421039 170944 0 None -7 2 Human 6.8 pIC50 = 6.8 Functional
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
ChEMBL 585 7 3 4 6.0 O=C(NCCO)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
23598642 161583 0 None -2 2 Human 5.8 pIC50 = 5.8 Functional
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
ChEMBL 541 6 2 3 7.1 CNCC1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
CHEMBL400267 161583 0 None -2 2 Human 5.8 pIC50 = 5.8 Functional
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
ChEMBL 541 6 2 3 7.1 CNCC1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
23598641 101052 0 None -6 2 Human 6.7 pIC50 = 6.7 Functional
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
ChEMBL 528 5 2 3 6.9 O=C(Nc1ccc(C(=O)N2CCC3(C=C(CO)CC3)Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2007.09.059
CHEMBL250346 101052 0 None -6 2 Human 6.7 pIC50 = 6.7 Functional
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
ChEMBL 528 5 2 3 6.9 O=C(Nc1ccc(C(=O)N2CCC3(C=C(CO)CC3)Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2007.09.059
44336784 115985 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
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
ChEMBL 626 9 2 4 7.0 CN(C)CCCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL321656 115985 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
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
ChEMBL 626 9 2 4 7.0 CN(C)CCCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
135192997 180609 0 None -489 4 Human 4.7 pIC50 = 4.7 Functional
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
ChEMBL 461 8 0 7 3.7 COc1ccc(-n2c(COCCF)nnc2N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)cn1 10.1021/acsmedchemlett.9b00186
CHEMBL4538696 180609 0 None -489 4 Human 4.7 pIC50 = 4.7 Functional
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
ChEMBL 461 8 0 7 3.7 COc1ccc(-n2c(COCCF)nnc2N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)cn1 10.1021/acsmedchemlett.9b00186
168294659 199180 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin-induced cAMP accumulation incubated for 1 hrAntagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin-induced cAMP accumulation incubated for 1 hr
ChEMBL 574 8 1 5 6.2 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
CHEMBL5207885 199180 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin-induced cAMP accumulation incubated for 1 hrAntagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin-induced cAMP accumulation incubated for 1 hr
ChEMBL 574 8 1 5 6.2 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
135192979 182617 0 None -125 4 Human 4.6 pIC50 = 4.6 Functional
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
ChEMBL 485 7 0 8 3.5 COc1ccc(-n2c(CO[C@H]3CCOC3)nnc2N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)cn1 10.1021/acsmedchemlett.9b00186
CHEMBL4585239 182617 0 None -125 4 Human 4.6 pIC50 = 4.6 Functional
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
ChEMBL 485 7 0 8 3.5 COc1ccc(-n2c(CO[C@H]3CCOC3)nnc2N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)cn1 10.1021/acsmedchemlett.9b00186
135192928 181683 0 None -851 4 Human 4.6 pIC50 = 4.6 Functional
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
ChEMBL 429 6 0 7 3.4 COCc1nnc(N2C[C@@H]3C[C@]3(c3cccc(F)c3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acsmedchemlett.9b00186
CHEMBL4564411 181683 0 None -851 4 Human 4.6 pIC50 = 4.6 Functional
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
ChEMBL 429 6 0 7 3.4 COCc1nnc(N2C[C@@H]3C[C@]3(c3cccc(F)c3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acsmedchemlett.9b00186
11683187 206711 44 None -20 2 Human 5.6 pIC50 = 5.6 Functional
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
ChEMBL 419 7 0 8 2.9 COCc1nnc(N2CC(Oc3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acs.jmedchem.8b00697
CHEMBL594828 206711 44 None -20 2 Human 5.6 pIC50 = 5.6 Functional
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
ChEMBL 419 7 0 8 2.9 COCc1nnc(N2CC(Oc3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acs.jmedchem.8b00697
11157078 100970 7 None -2 4 Rat 7.5 pIC50 = 7.5 Functional
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
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL249741 100970 7 None -2 4 Rat 7.5 pIC50 = 7.5 Functional
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
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
44352804 25731 0 None 24 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 536 7 2 4 7.0 O=C(O)CC[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL128688 25731 0 None 24 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 536 7 2 4 7.0 O=C(O)CC[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
9828129 123399 0 None 91 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 522 6 2 4 6.6 O=C(O)C[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL336825 123399 0 None 91 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 522 6 2 4 6.6 O=C(O)C[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
44336379 114194 0 None -6 2 Human 7.5 pIC50 = 7.5 Functional
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
ChEMBL 582 8 2 4 5.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCCN(C)C)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL318083 114194 0 None -6 2 Human 7.5 pIC50 = 7.5 Functional
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
ChEMBL 582 8 2 4 5.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCCN(C)C)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
135192983 182897 14 None -2137 4 Human 4.5 pIC50 = 4.5 Functional
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
ChEMBL 429 6 0 7 3.4 COCc1nnc(N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acsmedchemlett.9b00186
CHEMBL4591825 182897 14 None -2137 4 Human 4.5 pIC50 = 4.5 Functional
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
ChEMBL 429 6 0 7 3.4 COCc1nnc(N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acsmedchemlett.9b00186
44377836 64307 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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.
ChEMBL 505 4 2 2 7.3 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL166261 64307 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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.
ChEMBL 505 4 2 2 7.3 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
44336768 170131 0 None -1 2 Human 6.5 pIC50 = 6.5 Functional
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
ChEMBL 599 7 3 4 6.1 O=C(O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL419183 170131 0 None -1 2 Human 6.5 pIC50 = 6.5 Functional
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
ChEMBL 599 7 3 4 6.1 O=C(O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
44444762 161508 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
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
ChEMBL 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 10.1016/j.bmcl.2007.09.059
CHEMBL399888 161508 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
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
ChEMBL 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 10.1016/j.bmcl.2007.09.059
54582950 69811 0 None -3 4 Human 7.4 pIC50 = 7.4 Functional
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
ChEMBL 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 10.1016/j.bmcl.2004.04.016
CHEMBL1788220 69811 0 None -3 4 Human 7.4 pIC50 = 7.4 Functional
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
ChEMBL 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 10.1016/j.bmcl.2004.04.016
44352757 125232 0 None 58 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 522 6 2 4 6.6 O=C(O)C[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL341173 125232 0 None 58 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 522 6 2 4 6.6 O=C(O)C[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
23598595 161582 0 None -2 2 Human 6.4 pIC50 = 6.4 Functional
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
ChEMBL 542 5 2 3 7.0 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
CHEMBL400266 161582 0 None -2 2 Human 6.4 pIC50 = 6.4 Functional
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
ChEMBL 542 5 2 3 7.0 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
25132666 101304 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
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
ChEMBL 572 5 2 6 5.7 COc1cc(C(=O)N2CC[C@]3(C=C(c4nnn[nH]4)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL251715 101304 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
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
ChEMBL 572 5 2 6 5.7 COc1cc(C(=O)N2CC[C@]3(C=C(c4nnn[nH]4)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
44352768 122034 0 None 47 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 536 7 2 4 7.0 O=C(O)CC[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL334777 122034 0 None 47 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 536 7 2 4 7.0 O=C(O)CC[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
9871426 123789 0 None 44 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 522 6 2 4 6.6 O=C(O)CC1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL338901 123789 0 None 44 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 522 6 2 4 6.6 O=C(O)CC1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
44444760 161398 0 None -1 2 Human 6.4 pIC50 = 6.4 Functional
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
ChEMBL 518 4 2 3 6.1 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3Cl)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
CHEMBL399288 161398 0 None -1 2 Human 6.4 pIC50 = 6.4 Functional
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
ChEMBL 518 4 2 3 6.1 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3Cl)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
44336418 114964 0 None -2 2 Human 6.4 pIC50 = 6.4 Functional
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
ChEMBL 569 6 2 5 5.0 COC(=O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3C)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL319636 114964 0 None -2 2 Human 6.4 pIC50 = 6.4 Functional
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
ChEMBL 569 6 2 5 5.0 COC(=O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3C)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
10345610 72838 0 None -204 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human V2 receptorAntagonist activity at human V2 receptor
ChEMBL 422 2 0 6 3.6 CC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
CHEMBL1837040 72838 0 None -204 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human V2 receptorAntagonist activity at human V2 receptor
ChEMBL 422 2 0 6 3.6 CC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
23598598 11739 0 None 1 2 Human 7.3 pIC50 = 7.3 Functional
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
ChEMBL 608 7 2 4 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL104839 11739 0 None 1 2 Human 7.3 pIC50 = 7.3 Functional
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
ChEMBL 608 7 2 4 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
23598600 12139 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
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
ChEMBL 594 7 2 4 5.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL106938 12139 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
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
ChEMBL 594 7 2 4 5.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
172997 9112 57 None -4 5 Human 8.3 pIC50 = 8.3 Functional
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.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)01059-4
2238 9112 57 None -4 5 Human 8.3 pIC50 = 8.3 Functional
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.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)01059-4
CHEMBL49429 9112 57 None -4 5 Human 8.3 pIC50 = 8.3 Functional
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.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)01059-4
DB06666 9112 57 None -4 5 Human 8.3 pIC50 = 8.3 Functional
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.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)01059-4
11157078 100970 7 None -3 4 Human 7.3 pIC50 = 7.3 Functional
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
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL249741 100970 7 None -3 4 Human 7.3 pIC50 = 7.3 Functional
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
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
9937535 69812 1 None -26 4 Human 6.2 pIC50 = 6.2 Functional
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
ChEMBL 554 7 2 4 5.1 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL1788221 69812 1 None -26 4 Human 6.2 pIC50 = 6.2 Functional
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
ChEMBL 554 7 2 4 5.1 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
9826033 64236 0 None -37 3 Human 7.2 pIC50 = 7.2 Functional
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.
ChEMBL 471 4 2 2 6.7 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL165670 64236 0 None -37 3 Human 7.2 pIC50 = 7.2 Functional
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.
ChEMBL 471 4 2 2 6.7 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
9869993 172331 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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.
ChEMBL 485 4 2 2 7.0 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3CCCc4c[nH]c5cccc3c45)cc2)cc1 10.1016/s0960-894x(02)01059-4
CHEMBL424183 172331 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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.
ChEMBL 485 4 2 2 7.0 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3CCCc4c[nH]c5cccc3c45)cc2)cc1 10.1016/s0960-894x(02)01059-4
10456892 72839 0 None -74 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human V2 receptorAntagonist activity at human V2 receptor
ChEMBL 458 3 0 7 3.0 CS(=O)(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
CHEMBL1837041 72839 0 None -74 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human V2 receptorAntagonist activity at human V2 receptor
ChEMBL 458 3 0 7 3.0 CS(=O)(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
25133001 101273 0 None -7 2 Human 6.1 pIC50 = 6.1 Functional
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
ChEMBL 570 5 2 4 6.9 COc1cc(C(=O)N2CC[C@]3(C=C(c4ncc[nH]4)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL251561 101273 0 None -7 2 Human 6.1 pIC50 = 6.1 Functional
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
ChEMBL 570 5 2 4 6.9 COc1cc(C(=O)N2CC[C@]3(C=C(c4ncc[nH]4)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
135192932 178307 0 None -794 4 Human 5.1 pIC50 = 5.1 Functional
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
ChEMBL 443 7 0 7 3.8 CCOCc1nnc(N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acsmedchemlett.9b00186
CHEMBL4464246 178307 0 None -794 4 Human 5.1 pIC50 = 5.1 Functional
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
ChEMBL 443 7 0 7 3.8 CCOCc1nnc(N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acsmedchemlett.9b00186
46890707 13499 0 None -20 2 Human 6.1 pIC50 = 6.1 Functional
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
ChEMBL 419 3 0 3 6.6 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1csc2ccccc12 10.1016/j.bmcl.2010.04.068
CHEMBL1083703 13499 0 None -20 2 Human 6.1 pIC50 = 6.1 Functional
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
ChEMBL 419 3 0 3 6.6 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1csc2ccccc12 10.1016/j.bmcl.2010.04.068
11237434 72834 10 None -102 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human V2 receptorAntagonist activity at human V2 receptor
ChEMBL 394 2 0 6 3.6 CN1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
CHEMBL1837037 72834 10 None -102 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human V2 receptorAntagonist activity at human V2 receptor
ChEMBL 394 2 0 6 3.6 CN1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
23598598 11739 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human V2 receptor (Compound 7o)Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human V2 receptor (Compound 7o)
ChEMBL 608 7 2 4 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL104839 11739 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human V2 receptor (Compound 7o)Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human V2 receptor (Compound 7o)
ChEMBL 608 7 2 4 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
168294720 199248 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin-induced cAMP accumulation incubated for 1 hrAntagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin-induced cAMP accumulation incubated for 1 hr
ChEMBL 601 9 1 5 6.5 CCN1CCN(CCCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccccc32)CC1 10.1021/acs.jmedchem.2c00567
CHEMBL5208751 199248 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin-induced cAMP accumulation incubated for 1 hrAntagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin-induced cAMP accumulation incubated for 1 hr
ChEMBL 601 9 1 5 6.5 CCN1CCN(CCCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccccc32)CC1 10.1021/acs.jmedchem.2c00567
172997 9112 57 None -4 5 Human 7.0 pIC50 = 7.0 Functional
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.09.059
2238 9112 57 None -4 5 Human 7.0 pIC50 = 7.0 Functional
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.09.059
CHEMBL49429 9112 57 None -4 5 Human 7.0 pIC50 = 7.0 Functional
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.09.059
DB06666 9112 57 None -4 5 Human 7.0 pIC50 = 7.0 Functional
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.09.059
172997 9112 57 None -4 5 Human 7.0 pIC50 = 7.0 Functional
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.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)01059-4
2238 9112 57 None -4 5 Human 7.0 pIC50 = 7.0 Functional
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.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)01059-4
CHEMBL49429 9112 57 None -4 5 Human 7.0 pIC50 = 7.0 Functional
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.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)01059-4
DB06666 9112 57 None -4 5 Human 7.0 pIC50 = 7.0 Functional
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.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)01059-4
164946750 196905 1 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 minsAntagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
ChEMBL 574 8 2 5 6.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5173331 196905 1 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 minsAntagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
ChEMBL 574 8 2 5 6.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
44335330 166844 0 None - 0 Rat 8.0 pKd = 8.0 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1181 36 13 13 -2.0 CCOc1ccc(C[C@@H](NC(=O)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
CHEMBL410838 166844 0 None - 0 Rat 8.0 pKd = 8.0 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1181 36 13 13 -2.0 CCOc1ccc(C[C@@H](NC(=O)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
71458135 86464 0 None - 0 Pig 7.0 pKd = 7 Functional
Binding affinity towards V2-receptor in LLCPK cellsBinding affinity towards V2-receptor in LLCPK cells
ChEMBL 1171 20 11 15 1.3 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(N=[N+]=[N-])cc2)NC(=O)C(C)(C)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00079a020
CHEMBL2115364 86464 0 None - 0 Pig 7.0 pKd = 7 Functional
Binding affinity towards V2-receptor in LLCPK cellsBinding affinity towards V2-receptor in LLCPK cells
ChEMBL 1171 20 11 15 1.3 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(N=[N+]=[N-])cc2)NC(=O)C(C)(C)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00079a020
CHEMBL2373423 217156 0 None - 0 Rat 7.0 pKd = 7 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL None None None COc1ccc(C[C@@H](NC(=O)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
44335436 103834 0 None - 0 Rat 7.9 pKd = 7.9 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1161 35 13 13 -1.8 CCOc1ccc(C[C@@H](NC(=O)CC(C)(C)C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
CHEMBL267111 103834 0 None - 0 Rat 7.9 pKd = 7.9 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1161 35 13 13 -1.8 CCOc1ccc(C[C@@H](NC(=O)CC(C)(C)C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
44335358 162776 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00173a027
CHEMBL406184 162776 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00173a027
CHEMBL2370376 216619 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL None None None CCOc1ccc(C[C@@H](NC(=O)CC23CC4CC(CC(C4)C2)C3)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
CHEMBL2370381 216621 0 None - 0 Rat 7.7 pKd = 7.7 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL None None None CCOc1ccc(C[C@@H](NC(=O)CC23CC4CC(CC(C4)C2)C3)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
CHEMBL2370380 216620 0 None - 0 Rat 7.7 pKd = 7.7 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)CC12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00173a027
14730755 104100 0 None - 0 Rat 6.6 pKd = 6.6 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1064 32 12 12 -1.8 CCOc1ccc(C[C@@H](NC(=O)CC(C)(C)C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(C)[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
CHEMBL269251 104100 0 None - 0 Rat 6.6 pKd = 6.6 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1064 32 12 12 -1.8 CCOc1ccc(C[C@@H](NC(=O)CC(C)(C)C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(C)[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
CHEMBL2373516 217159 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL None None None CCOc1ccc(C[C@@H](NC(=O)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
44335434 167420 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1083 30 10 11 0.9 CCOc1ccc(C[C@@H](NC(=O)CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
CHEMBL411320 167420 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1083 30 10 11 0.9 CCOc1ccc(C[C@@H](NC(=O)CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
CHEMBL2373374 217155 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL None None None NCCCC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)Cc1ccccc1)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00173a027
CHEMBL2373441 217157 0 None - 0 Rat 5.2 pKd = 5.2 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL None None None CCOc1ccc(C[C@@H](NC(=O)CC(C)(C)C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm00173a027
44335231 164341 0 None - 0 Rat 8.1 pKd = 8.1 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1239 36 13 13 -0.6 CCOc1ccc(C[C@@H](NC(=O)CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
CHEMBL408038 164341 0 None - 0 Rat 8.1 pKd = 8.1 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1239 36 13 13 -0.6 CCOc1ccc(C[C@@H](NC(=O)CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
44385657 175006 0 None - 0 Pig 8.9 pKi = 8.9 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 967 16 10 12 0.8 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL433614 175006 0 None - 0 Pig 8.9 pKi = 8.9 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 967 16 10 12 0.8 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL2372280 216987 0 None - 0 Pig 8.8 pKi = 8.8 Functional
In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pigIn vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pig
ChEMBL None None None CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSCC(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00403a001
44579442 193607 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 391 7 0 9 2.7 CCOc1ccc(-c2nnc(Cn3nccn3)n2-c2ccc(OC)nc2)cc1C 10.1016/j.bmcl.2008.08.066
CHEMBL489387 193607 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 391 7 0 9 2.7 CCOc1ccc(-c2nnc(Cn3nccn3)n2-c2ccc(OC)nc2)cc1C 10.1016/j.bmcl.2008.08.066
11384094 185362 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at vasopressin V2 receptorAntagonist activity at vasopressin V2 receptor
ChEMBL 402 6 0 8 3.6 COCc1nnc(-c2cnc(-c3cccc(C)c3C)cn2)n1-c1ccc(OC)nc1 10.1016/j.bmcl.2008.06.098
CHEMBL467186 185362 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at vasopressin V2 receptorAntagonist activity at vasopressin V2 receptor
ChEMBL 402 6 0 8 3.6 COCc1nnc(-c2cnc(-c3cccc(C)c3C)cn2)n1-c1ccc(OC)nc1 10.1016/j.bmcl.2008.06.098
44325538 119338 0 None - 0 Human 8.0 pKi = 8.0 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccc(O)cc1 10.1016/j.bmcl.2004.03.083
CHEMBL330016 119338 0 None - 0 Human 8.0 pKi = 8.0 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccc(O)cc1 10.1016/j.bmcl.2004.03.083
46225153 205890 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta lactamase assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta lactamase assay
ChEMBL 399 7 0 8 2.5 COCc1nnc(N2CC(Oc3ccc(F)cc3C)C2)n1-c1ccc(OC)nc1 10.1016/j.bmcl.2009.11.097
CHEMBL589128 205890 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta lactamase assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta lactamase assay
ChEMBL 399 7 0 8 2.5 COCc1nnc(N2CC(Oc3ccc(F)cc3C)C2)n1-c1ccc(OC)nc1 10.1016/j.bmcl.2009.11.097
44325345 118339 0 None - 0 Human 7.9 pKi = 7.9 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 493 3 1 4 4.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2004.03.083
CHEMBL328079 118339 0 None - 0 Human 7.9 pKi = 7.9 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 493 3 1 4 4.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2004.03.083
44325505 214222 0 None - 0 Human 7.9 pKi = 7.9 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1cc(F)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL94133 214222 0 None - 0 Human 7.9 pKi = 7.9 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1cc(F)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44581241 182665 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assayAntagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assay
ChEMBL 495 8 0 6 5.2 COc1ccc(S(=O)(=O)N(Cc2ccc(-c3ccccc3Cl)cn2)c2ccc(OC)nc2)cc1 10.1016/j.bmcl.2008.11.018
CHEMBL458634 182665 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assayAntagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assay
ChEMBL 495 8 0 6 5.2 COc1ccc(S(=O)(=O)N(Cc2ccc(-c3ccccc3Cl)cn2)c2ccc(OC)nc2)cc1 10.1016/j.bmcl.2008.11.018
44386688 139347 0 None - 0 Pig 7.9 pKi = 7.9 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 981 17 10 12 1.2 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL369806 139347 0 None - 0 Pig 7.9 pKi = 7.9 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 981 17 10 12 1.2 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
10414302 119297 0 None - 0 Human 7.8 pKi = 7.8 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2C[C@H]3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL329903 119297 0 None - 0 Human 7.8 pKi = 7.8 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2C[C@H]3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325332 214170 0 None - 0 Human 7.8 pKi = 7.8 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 503 4 1 4 5.5 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL93861 214170 0 None - 0 Human 7.8 pKi = 7.8 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 503 4 1 4 5.5 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44577937 185361 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at vasopressin V2 receptorAntagonist activity at vasopressin V2 receptor
ChEMBL 402 7 0 7 4.2 COCc1nnc(-c2ccc(-c3ccccc3OC)cc2)n1-c1ccc(OC)nc1 10.1016/j.bmcl.2008.06.098
CHEMBL467185 185361 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at vasopressin V2 receptorAntagonist activity at vasopressin V2 receptor
ChEMBL 402 7 0 7 4.2 COCc1nnc(-c2ccc(-c3ccccc3OC)cc2)n1-c1ccc(OC)nc1 10.1016/j.bmcl.2008.06.098
44325691 19770 0 None - 0 Human 7.8 pKi = 7.8 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 1 4 6.8 O=C(Nc1ccc(C(=O)N2C[C@H]3CSCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL1189693 19770 0 None - 0 Human 7.8 pKi = 7.8 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 1 4 6.8 O=C(Nc1ccc(C(=O)N2C[C@H]3CSCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL539285 19770 0 None - 0 Human 7.8 pKi = 7.8 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 1 4 6.8 O=C(Nc1ccc(C(=O)N2C[C@H]3CSCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
9807250 85122 0 None - 0 Human 6.8 pKi = 6.8 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 O=C(Nc1ccc(C(=O)N2C[C@@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL2093899 85122 0 None - 0 Human 6.8 pKi = 6.8 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 O=C(Nc1ccc(C(=O)N2C[C@@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL2110044 85122 0 None - 0 Human 6.8 pKi = 6.8 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 O=C(Nc1ccc(C(=O)N2C[C@@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325695 174785 0 None - 0 Human 8.7 pKi = 8.7 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1cccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c1 10.1016/j.bmcl.2004.03.083
CHEMBL432043 174785 0 None - 0 Human 8.7 pKi = 8.7 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1cccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c1 10.1016/j.bmcl.2004.03.083
44325362 214123 0 None - 0 Human 8.7 pKi = 8.7 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccc(F)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL93603 214123 0 None - 0 Human 8.7 pKi = 8.7 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccc(F)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44386594 134979 0 None - 0 Pig 8.6 pKi = 8.6 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 967 16 10 12 0.8 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL366552 134979 0 None - 0 Pig 8.6 pKi = 8.6 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 967 16 10 12 0.8 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
44386593 165225 0 None - 0 Pig 8.6 pKi = 8.6 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1024 18 11 13 -0.1 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL409054 165225 0 None - 0 Pig 8.6 pKi = 8.6 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1024 18 11 13 -0.1 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
73354746 96254 0 None - 0 Pig 8.5 pKi = 8.5 Functional
In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pigIn vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pig
ChEMBL 981 16 10 12 0.3 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSCC(C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00403a001
CHEMBL2372281 96254 0 None - 0 Pig 8.5 pKi = 8.5 Functional
In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pigIn vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pig
ChEMBL 981 16 10 12 0.3 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSCC(C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00403a001
9849525 118203 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL327365 118203 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325558 119346 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1cccc(O)c1 10.1016/j.bmcl.2004.03.083
CHEMBL330094 119346 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1cccc(O)c1 10.1016/j.bmcl.2004.03.083
172997 9112 57 None -4 5 Human 7.6 pKi = 7.6 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2004.03.083
2238 9112 57 None -4 5 Human 7.6 pKi = 7.6 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2004.03.083
CHEMBL49429 9112 57 None -4 5 Human 7.6 pKi = 7.6 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2004.03.083
DB06666 9112 57 None -4 5 Human 7.6 pKi = 7.6 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2004.03.083
44325804 214089 0 None - 0 Human 7.6 pKi = 7.6 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 533 4 1 4 6.5 Cc1ccc2c(c1)N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)CC1CSCCN1C2 10.1016/j.bmcl.2004.03.083
CHEMBL93366 214089 0 None - 0 Human 7.6 pKi = 7.6 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 533 4 1 4 6.5 Cc1ccc2c(c1)N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)CC1CSCCN1C2 10.1016/j.bmcl.2004.03.083
44386687 134683 0 None - 0 Pig 7.6 pKi = 7.6 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 968 16 10 12 1.4 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL366473 134683 0 None - 0 Pig 7.6 pKi = 7.6 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 968 16 10 12 1.4 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
46830095 15035 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 376 5 0 5 4.2 COc1ccc(N(C(=O)c2cnc(-c3cccc(C)c3C)cn2)C(C)C)cn1 10.1016/j.bmcl.2010.02.018
CHEMBL1092459 15035 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 376 5 0 5 4.2 COc1ccc(N(C(=O)c2cnc(-c3cccc(C)c3C)cn2)C(C)C)cn1 10.1016/j.bmcl.2010.02.018
46830094 15206 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 392 7 0 6 3.5 COCCN(C(=O)c1cnc(-c2cccc(C)c2C)cn1)c1ccc(OC)nc1 10.1016/j.bmcl.2010.02.018
CHEMBL1093599 15206 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 392 7 0 6 3.5 COCCN(C(=O)c1cnc(-c2cccc(C)c2C)cn1)c1ccc(OC)nc1 10.1016/j.bmcl.2010.02.018
44581242 182666 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assayAntagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assay
ChEMBL 475 8 0 6 4.9 COc1ccc(S(=O)(=O)N(Cc2ccc(-c3ccccc3C)cn2)c2ccc(OC)nc2)cc1 10.1016/j.bmcl.2008.11.018
CHEMBL458635 182666 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assayAntagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assay
ChEMBL 475 8 0 6 4.9 COc1ccc(S(=O)(=O)N(Cc2ccc(-c3ccccc3C)cn2)c2ccc(OC)nc2)cc1 10.1016/j.bmcl.2008.11.018
46225118 207831 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta lactamase assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta lactamase assay
ChEMBL 369 5 0 7 2.7 COc1ccc(-n2c(C)nnc2N2CC(Oc3cc(F)ccc3C)C2)cn1 10.1016/j.bmcl.2009.11.097
CHEMBL602641 207831 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta lactamase assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta lactamase assay
ChEMBL 369 5 0 7 2.7 COc1ccc(-n2c(C)nnc2N2CC(Oc3cc(F)ccc3C)C2)cn1 10.1016/j.bmcl.2009.11.097
46830096 14768 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 362 5 0 5 3.8 CCN(C(=O)c1cnc(-c2cccc(C)c2C)cn1)c1ccc(OC)nc1 10.1016/j.bmcl.2010.02.018
CHEMBL1090654 14768 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 362 5 0 5 3.8 CCN(C(=O)c1cnc(-c2cccc(C)c2C)cn1)c1ccc(OC)nc1 10.1016/j.bmcl.2010.02.018
44325607 118933 0 None - 0 Human 8.5 pKi = 8.5 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)cc1 10.1016/j.bmcl.2004.03.083
CHEMBL329026 118933 0 None - 0 Human 8.5 pKi = 8.5 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)cc1 10.1016/j.bmcl.2004.03.083
CHEMBL2372316 216995 0 None - 0 Pig 8.5 pKi = 8.5 Functional
In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pigIn vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pig
ChEMBL None None None CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)CCCC(C(=O)N3CCC[C@@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00403a001
CHEMBL2372291 216990 0 None - 0 Pig 8.4 pKi = 8.4 Functional
In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pigIn vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pig
ChEMBL None None None CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSCC(C(=O)N3CCC[C@@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00403a001
44382370 148328 0 None - 0 Pig 8.4 pKi = 8.4 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL384776 148328 0 None - 0 Pig 8.4 pKi = 8.4 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
44325915 119515 0 None - 0 Human 6.5 pKi = 6.5 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 509 3 1 4 5.6 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2004.03.083
CHEMBL330494 119515 0 None - 0 Human 6.5 pKi = 6.5 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 509 3 1 4 5.6 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2004.03.083
2198 10193 2 None - 0 Human 8.4 pKi = 8.4 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 Clc1cc(ccc1C(=O)N1C[C@H]2COCCN2Cc2c1cccc2)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2004.03.083
9807249 10193 2 None - 0 Human 8.4 pKi = 8.4 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 Clc1cc(ccc1C(=O)N1C[C@H]2COCCN2Cc2c1cccc2)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL1192593 10193 2 None - 0 Human 8.4 pKi = 8.4 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 Clc1cc(ccc1C(=O)N1C[C@H]2COCCN2Cc2c1cccc2)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2004.03.083
44325896 214590 0 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 551 4 1 5 4.9 O=C(Nc1ccc(C(=O)N2CC3CS(=O)(=O)CCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL96255 214590 0 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 551 4 1 5 4.9 O=C(Nc1ccc(C(=O)N2CC3CS(=O)(=O)CCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325895 214687 0 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2C[C@@H]3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL96731 214687 0 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2C[C@@H]3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44385658 165631 0 None - 0 Pig 7.4 pKi = 7.4 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1025 18 11 13 0.5 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(=O)O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL409486 165631 0 None - 0 Pig 7.4 pKi = 7.4 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1025 18 11 13 0.5 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(=O)O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
44325363 113387 0 None - 0 Human 8.3 pKi = 8.3 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c(-c2ccccc2)c1 10.1016/j.bmcl.2004.03.083
CHEMBL314290 113387 0 None - 0 Human 8.3 pKi = 8.3 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c(-c2ccccc2)c1 10.1016/j.bmcl.2004.03.083
73348612 96242 0 None - 0 Pig 8.2 pKi = 8.2 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 939 16 9 12 1.9 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL2371680 96242 0 None - 0 Pig 8.2 pKi = 8.2 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 939 16 9 12 1.9 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
44577936 185360 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at vasopressin V2 receptorAntagonist activity at vasopressin V2 receptor
ChEMBL 371 5 0 5 4.9 COc1ccc(-n2c(C)nnc2-c2ccc(-c3ccccc3OC)cc2)cc1 10.1016/j.bmcl.2008.06.098
CHEMBL467184 185360 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at vasopressin V2 receptorAntagonist activity at vasopressin V2 receptor
ChEMBL 371 5 0 5 4.9 COc1ccc(-n2c(C)nnc2-c2ccc(-c3ccccc3OC)cc2)cc1 10.1016/j.bmcl.2008.06.098
44581240 196503 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assayAntagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assay
ChEMBL 486 8 0 7 4.4 COc1ccc(S(=O)(=O)N(Cc2ccc(-c3ccccc3C#N)cn2)c2ccc(OC)nc2)cc1 10.1016/j.bmcl.2008.11.018
CHEMBL515660 196503 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assayAntagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assay
ChEMBL 486 8 0 7 4.4 COc1ccc(S(=O)(=O)N(Cc2ccc(-c3ccccc3C#N)cn2)c2ccc(OC)nc2)cc1 10.1016/j.bmcl.2008.11.018
44325703 118180 0 None - 0 Human 8.2 pKi = 8.2 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccc(O)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL327242 118180 0 None - 0 Human 8.2 pKi = 8.2 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccc(O)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44375638 175627 0 None - 0 Pig 8.2 pKi = 8.2 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL438014 175627 0 None - 0 Pig 8.2 pKi = 8.2 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
44581266 182174 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assayAntagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assay
ChEMBL 479 8 0 6 4.7 COc1ccc(S(=O)(=O)N(Cc2ccc(-c3ccccc3F)cn2)c2ccc(OC)nc2)cc1 10.1016/j.bmcl.2008.11.018
CHEMBL457544 182174 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assayAntagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assay
ChEMBL 479 8 0 6 4.7 COc1ccc(S(=O)(=O)N(Cc2ccc(-c3ccccc3F)cn2)c2ccc(OC)nc2)cc1 10.1016/j.bmcl.2008.11.018
11486351 199756 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity at human vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 398 10 0 8 3.2 CCOc1ccc(-c2nnc(COCCOC)n2-c2ccc(OC)nc2)cc1C 10.1016/j.bmcl.2008.08.066
CHEMBL522255 199756 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity at human vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 398 10 0 8 3.2 CCOc1ccc(-c2nnc(COCCOC)n2-c2ccc(OC)nc2)cc1C 10.1016/j.bmcl.2008.08.066
44325704 119084 0 None - 0 Human 7.2 pKi = 7.2 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1cc(O)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL329141 119084 0 None - 0 Human 7.2 pKi = 7.2 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1cc(O)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325905 171056 0 None - 0 Human 7.2 pKi = 7.2 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 571 4 1 4 7.0 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1)c1cc(F)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL421180 171056 0 None - 0 Human 7.2 pKi = 7.2 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 571 4 1 4 7.0 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1)c1cc(F)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
2042 9757 58 None -26 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central None None None None None
2174 9757 58 None -26 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central None None None None None
2176 9757 58 None -26 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central None None None None None
439302 9757 58 None -26 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central None None None None None
CHEMBL395429 9757 58 None -26 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central None None None None None
DB00107 9757 58 None -26 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central None None None None None
5280343 195054 124 None -31 12 Human 8.3 pIC50 = 8.3 Functional
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
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 195054 124 None -31 12 Human 8.3 pIC50 = 8.3 Functional
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
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 195054 124 None -31 12 Human 8.3 pIC50 = 8.3 Functional
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
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
2812 11551 101 None -16 44 Human 8.3 pIC50 = 8.3 Functional
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
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 11551 101 None -16 44 Human 8.3 pIC50 = 8.3 Functional
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
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
3793 209988 77 None -2 4 Human 8.2 pIC50 = 8.2 Functional
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
Drug Central 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O None
45039617 209988 77 None -2 4 Human 8.2 pIC50 = 8.2 Functional
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
Drug Central 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O None
CHEMBL64391 209988 77 None -2 4 Human 8.2 pIC50 = 8.2 Functional
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
Drug Central 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O None
3537 10776 22 None 3 4 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 16297621
5311500 10776 22 None 3 4 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 16297621
CHEMBL363910 10776 22 None 3 4 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 16297621




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
3686 101442 108 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 338 12 1 5 3.5 COC1=C(OC)C(=O)C(CCCCCCCCCCO)=C(C)C1=O 10.1038/s41467-023-40064-9
CHEMBL252556 101442 108 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 338 12 1 5 3.5 COC1=C(OC)C(=O)C(CCCCCCCCCCO)=C(C)C1=O 10.1038/s41467-023-40064-9
2335 18620 22 None - 12 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
8478 18620 22 None - 12 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 18620 22 None - 12 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL221753 18620 22 None - 12 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
41684 37995 105 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
CHEMBL1401 37995 105 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
2600 10551 74 None - 13 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 10551 74 None - 13 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 10551 74 None - 13 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 10551 74 None - 13 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 10551 74 None - 13 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
216416 118358 48 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL328190 118358 48 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
107771 127026 49 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 517 7 2 7 6.1 COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1 10.1038/s41467-023-40064-9
CHEMBL35228 127026 49 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 517 7 2 7 6.1 COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1 10.1038/s41467-023-40064-9
214 10632 58 None - 30 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 10632 58 None - 30 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 10632 58 None - 30 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 10632 58 None - 30 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 10632 58 None - 30 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 10632 58 None - 30 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
156419 7725 74 None - 1 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
3308 7725 74 None - 1 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
647 7725 74 None - 1 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL1201284 7725 74 None - 1 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
DB01012 7725 74 None - 1 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
68617 212306 62 None - 26 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1709 212306 62 None - 26 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL809 212306 62 None - 26 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
212 10578 47 None - 25 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2639 10578 47 None - 25 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651 10578 47 None - 25 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL1201 10578 47 None - 25 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01623 10578 47 None - 25 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
135409453 10545 41 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 10545 41 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 10545 41 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
5328940 106992 107 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
CHEMBL288441 106992 107 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
9915743 70316 93 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 556 11 2 8 5.9 CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)/C=C/CN(C)C 10.1038/s41467-023-40064-9
CHEMBL180022 70316 93 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 556 11 2 8 5.9 CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)/C=C/CN(C)C 10.1038/s41467-023-40064-9
1222 8445 49 None - 32 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3396 8445 49 None - 32 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
85 8445 49 None - 32 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL46516 8445 49 None - 32 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
DB04842 8445 49 None - 32 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
16362 9899 71 None - 29 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2172 9899 71 None - 29 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
90 9899 71 None - 29 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1423 9899 71 None - 29 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01100 9899 71 None - 29 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
191 7191 98 None - 29 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 7191 98 None - 29 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 7191 98 None - 29 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 7191 98 None - 29 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 7191 98 None - 29 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
6436173 61890 45 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL1617 61890 45 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
4495 203314 92 None - 29 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL56367 203314 92 None - 29 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 10.1038/s41467-023-40064-9
2435 10362 83 None - 48 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
60149 10362 83 None - 48 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
98 10362 83 None - 48 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
CHEMBL12713 10362 83 None - 48 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
DB06144 10362 83 None - 48 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
176 7186 66 None - 31 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2157 7186 66 None - 31 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2566 7186 66 None - 31 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
CHEMBL633 7186 66 None - 31 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
DB01118 7186 66 None - 31 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
118422671 9533 65 None - 4 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
1887 9533 65 None - 4 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
189562 9533 65 None - 4 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
71301 9533 65 None - 4 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
7246 9533 65 None - 4 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
9844194 9533 65 None - 4 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL2365658 9533 65 None - 4 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL3526436 9533 65 None - 4 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL434394 9533 65 None - 4 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
DB04861 9533 65 None - 4 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
135398735 143746 32 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
136262914 143746 32 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL374478 143746 32 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
4046 9261 33 None - 2 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 9261 33 None - 2 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 9261 33 None - 2 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 9261 33 None - 2 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
21722 24764 31 None - 6 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
CHEMBL126224 24764 31 None - 6 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
54585 21274 85 None - 0 Human 4.4 pAC50 = 4.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 7 4 6 2.7 O=C(O)CCNC(=O)c1ccc(/N=N/c2ccc(O)c(C(=O)O)c2)cc1 10.1038/s41467-023-40064-9
CHEMBL1201346 21274 85 None - 0 Human 4.4 pAC50 = 4.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 7 4 6 2.7 O=C(O)CCNC(=O)c1ccc(/N=N/c2ccc(O)c(C(=O)O)c2)cc1 10.1038/s41467-023-40064-9
2213 7306 46 None -660 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
3008 7306 46 None -660 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
5311010 7306 46 None -660 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
68613 7306 46 None -660 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
CHEMBL378642 7306 46 None -660 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
CHEMBL382301 7306 46 None -660 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
DB09059 7306 46 None -660 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
2713 212050 82 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5353524 212050 82 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5360566 212050 82 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
88536661 212050 82 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
9552079 212050 82 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1330113 212050 82 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL790 212050 82 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5329102 201505 86 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 201505 86 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
11980903 21264 19 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
22526 21264 19 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
5281035 21264 19 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201303 21264 19 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
3149 19386 15 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1187011 19386 15 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
72093 41835 9 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL1433361 41835 9 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL2103773 41835 9 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
2168 10748 38 None -15 9 Human 10.3 pEC50 = 10.3 Binding
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
ChEMBL None None None None 10.1021/jm500365s
2810 10748 38 None -15 9 Human 10.3 pEC50 = 10.3 Binding
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
ChEMBL None None None None 10.1021/jm500365s
644077 10748 38 None -15 9 Human 10.3 pEC50 = 10.3 Binding
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
ChEMBL None None None None 10.1021/jm500365s
CHEMBL373742 10748 38 None -15 9 Human 10.3 pEC50 = 10.3 Binding
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
ChEMBL None None None None 10.1021/jm500365s
DB00067 10748 38 None -15 9 Human 10.3 pEC50 = 10.3 Binding
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
ChEMBL None None None None 10.1021/jm500365s
2181 8113 42 None -14 7 Human 9.7 pEC50 = 9.7 Binding
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
ChEMBL None None None None 10.1021/jm500365s
2182 8113 42 None -14 7 Human 9.7 pEC50 = 9.7 Binding
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
ChEMBL None None None None 10.1021/jm500365s
27991 8113 42 None -14 7 Human 9.7 pEC50 = 9.7 Binding
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
ChEMBL None None None None 10.1021/jm500365s
5311065 8113 42 None -14 7 Human 9.7 pEC50 = 9.7 Binding
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
ChEMBL None None None None 10.1021/jm500365s
CHEMBL1429 8113 42 None -14 7 Human 9.7 pEC50 = 9.7 Binding
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
ChEMBL None None None None 10.1021/jm500365s
CHEMBL264448 8113 42 None -14 7 Human 9.7 pEC50 = 9.7 Binding
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
ChEMBL None None None None 10.1021/jm500365s
DB00035 8113 42 None -14 7 Human 9.7 pEC50 = 9.7 Binding
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
ChEMBL None None None None 10.1021/jm500365s
118719821 122523 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353932 122523 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
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
ChEMBL 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 10.1021/jm500365s
118719829 122531 0 None - 0 Human 7.0 pEC50 = 7 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353940 122531 0 None - 0 Human 7.0 pEC50 = 7 Binding
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
ChEMBL 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 10.1021/jm500365s
118719832 122534 0 None - 0 Human 7.0 pEC50 = 7 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353943 122534 0 None - 0 Human 7.0 pEC50 = 7 Binding
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
ChEMBL 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 10.1021/jm500365s
118720286 122638 0 None - 0 Human 7.0 pEC50 = 7 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354598 122638 0 None - 0 Human 7.0 pEC50 = 7 Binding
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
ChEMBL 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 10.1021/jm500365s
44393912 71329 0 None - 0 Human 7.0 pEC50 = 7 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 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 10.1016/j.bmcl.2004.04.107
CHEMBL181487 71329 0 None - 0 Human 7.0 pEC50 = 7 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 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 10.1016/j.bmcl.2004.04.107
118720277 122627 0 None - 0 Human 6.0 pEC50 = 6 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354587 122627 0 None - 0 Human 6.0 pEC50 = 6 Binding
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
ChEMBL 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 10.1021/jm500365s
118719828 122530 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353939 122530 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
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
ChEMBL 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 10.1021/jm500365s
118720275 122625 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354585 122625 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
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
ChEMBL 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 10.1021/jm500365s
118720266 122617 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354577 122617 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
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
ChEMBL 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 10.1021/jm500365s
10282736 130593 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 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 10.1016/j.bmcl.2004.04.107
CHEMBL362382 130593 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 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 10.1016/j.bmcl.2004.04.107
118720274 122624 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354584 122624 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
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
ChEMBL 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 10.1021/jm500365s
44394045 176282 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 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 10.1016/j.bmcl.2004.04.107
CHEMBL443300 176282 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 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 10.1016/j.bmcl.2004.04.107
118720267 122618 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354578 122618 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
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
ChEMBL 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 10.1021/jm500365s
44393965 132980 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 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 10.1016/j.bmcl.2004.04.107
CHEMBL364994 132980 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 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 10.1016/j.bmcl.2004.04.107
118720278 122628 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354588 122628 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
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
ChEMBL 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 10.1021/jm500365s
118720284 122635 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354595 122635 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
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
ChEMBL 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 10.1021/jm500365s
118720262 122613 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354573 122613 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
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
ChEMBL 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 10.1021/jm500365s
118720263 122614 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354574 122614 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
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
ChEMBL 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 10.1021/jm500365s
118720285 122636 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354596 122636 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
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
ChEMBL 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 10.1021/jm500365s
118720269 122620 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354580 122620 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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
ChEMBL 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 10.1021/jm500365s
44232512 122637 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354597 122637 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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
ChEMBL 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 10.1021/jm500365s
118720283 122633 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354593 122633 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
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
ChEMBL 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 10.1021/jm500365s
11169 7584 37 None -1 2 Human 6.8 pEC50 = 6.8 Binding
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
ChEMBL 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 10.1021/jm500365s
131676677 7584 37 None -1 2 Human 6.8 pEC50 = 6.8 Binding
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
ChEMBL 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 10.1021/jm500365s
165708555 7584 37 None -1 2 Human 6.8 pEC50 = 6.8 Binding
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
ChEMBL 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 10.1021/jm500365s
16681432 7584 37 None -1 2 Human 6.8 pEC50 = 6.8 Binding
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
ChEMBL 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 10.1021/jm500365s
495 7584 37 None -1 2 Human 6.8 pEC50 = 6.8 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3301668 7584 37 None -1 2 Human 6.8 pEC50 = 6.8 Binding
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
ChEMBL 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 10.1021/jm500365s
DB01282 7584 37 None -1 2 Human 6.8 pEC50 = 6.8 Binding
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
ChEMBL 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 10.1021/jm500365s
118719840 122542 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353951 122542 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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
ChEMBL 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 10.1021/jm500365s
118720272 122622 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354582 122622 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
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
ChEMBL 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 10.1021/jm500365s
118719839 122541 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353950 122541 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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
ChEMBL 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 10.1021/jm500365s
118719843 122545 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353954 122545 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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
ChEMBL 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 10.1021/jm500365s
44393998 73049 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 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 10.1016/j.bmcl.2004.04.107
CHEMBL184696 73049 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 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 10.1016/j.bmcl.2004.04.107
44394063 73135 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 573 4 1 5 5.0 CN1CCCN(C(=S)[C@@H]2CCCN2C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)CC1 10.1016/j.bmcl.2004.04.107
CHEMBL185152 73135 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 573 4 1 5 5.0 CN1CCCN(C(=S)[C@@H]2CCCN2C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)CC1 10.1016/j.bmcl.2004.04.107
44393911 72000 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 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 10.1016/j.bmcl.2004.04.107
CHEMBL182627 72000 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 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 10.1016/j.bmcl.2004.04.107
118720273 122623 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354583 122623 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
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
ChEMBL 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 10.1021/jm500365s
118720281 122631 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354591 122631 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
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
ChEMBL 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 10.1021/jm500365s
118720276 122626 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354586 122626 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
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
ChEMBL 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 10.1021/jm500365s
118720261 122612 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354572 122612 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
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
ChEMBL 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 10.1021/jm500365s
44394044 130613 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 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 10.1016/j.bmcl.2004.04.107
CHEMBL362483 130613 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 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 10.1016/j.bmcl.2004.04.107
118720288 122640 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354600 122640 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
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
ChEMBL 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 10.1021/jm500365s
118720270 122292 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3352839 122292 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
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
ChEMBL 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 10.1021/jm500365s
449224 175754 12 None - 1 Human 8.5 pEC50 = 8.5 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL439044 175754 12 None - 1 Human 8.5 pEC50 = 8.5 Binding
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
ChEMBL 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 10.1021/jm500365s
118719835 122537 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353946 122537 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
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
ChEMBL 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 10.1021/jm500365s
118720289 122641 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354601 122641 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
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
ChEMBL 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 10.1021/jm500365s
118720287 122639 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354599 122639 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm500365s
76073634 122634 3 None - 1 Human 6.5 pEC50 = 6.5 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354594 122634 3 None - 1 Human 6.5 pEC50 = 6.5 Binding
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
ChEMBL 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 10.1021/jm500365s
118719833 122535 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353944 122535 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
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
ChEMBL 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 10.1021/jm500365s
118719820 122522 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353931 122522 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
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
ChEMBL 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 10.1021/jm500365s
118720279 122629 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354589 122629 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
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
ChEMBL 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 10.1021/jm500365s
2252 9011 48 None -10000 5 Human 4.4 pEC50 = 4.4 Binding
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
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1021/jm901084f
6918320 9011 48 None -10000 5 Human 4.4 pEC50 = 4.4 Binding
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
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1021/jm901084f
CHEMBL24781 9011 48 None -10000 5 Human 4.4 pEC50 = 4.4 Binding
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
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1021/jm901084f
118719841 122543 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353952 122543 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
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
ChEMBL 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 10.1021/jm500365s
3537 10776 22 None 3 3 Human 7.4 pEC50 = 7.4 Binding
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
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/jm901084f
5311500 10776 22 None 3 3 Human 7.4 pEC50 = 7.4 Binding
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
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/jm901084f
CHEMBL363910 10776 22 None 3 3 Human 7.4 pEC50 = 7.4 Binding
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
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/jm901084f
118719818 122520 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353929 122520 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
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
ChEMBL 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 10.1021/jm500365s
118719824 122526 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353935 122526 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
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
ChEMBL 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 10.1021/jm500365s
118719825 122527 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353936 122527 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
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
ChEMBL 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 10.1021/jm500365s
118719826 122528 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353937 122528 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
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
ChEMBL 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 10.1021/jm500365s
118719844 122546 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353955 122546 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
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
ChEMBL 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 10.1021/jm500365s
118720268 122619 0 None - 1 Human 6.3 pEC50 = 6.3 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354579 122619 0 None - 1 Human 6.3 pEC50 = 6.3 Binding
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
ChEMBL 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 10.1021/jm500365s
118720265 122616 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354576 122616 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
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
ChEMBL 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 10.1021/jm500365s
118720282 122632 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354592 122632 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
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
ChEMBL 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 10.1021/jm500365s
118719830 122532 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353941 122532 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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
ChEMBL 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 10.1021/jm500365s
118719845 122547 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353956 122547 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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
ChEMBL 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 10.1021/jm500365s
44393941 177627 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 595 8 2 6 4.4 CO[C@@H]1C[C@@H](C(=O)NCCc2ccccn2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1 10.1016/j.bmcl.2004.04.107
CHEMBL445393 177627 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 595 8 2 6 4.4 CO[C@@H]1C[C@@H](C(=O)NCCc2ccccn2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1 10.1016/j.bmcl.2004.04.107
118720259 122610 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354570 122610 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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
ChEMBL 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 10.1021/jm500365s
118719842 122544 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353953 122544 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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
ChEMBL 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 10.1021/jm500365s
118719823 122525 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353934 122525 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
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
ChEMBL 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 10.1021/jm500365s
118719834 122536 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353945 122536 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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
ChEMBL 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 10.1021/jm500365s
118719822 122524 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353933 122524 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
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
ChEMBL 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 10.1021/jm500365s
2042 9757 58 None -831 8 Human 8.1 pEC50 = 8.1 Binding
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
ChEMBL None None None None 10.1021/jm500365s
2174 9757 58 None -831 8 Human 8.1 pEC50 = 8.1 Binding
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
ChEMBL None None None None 10.1021/jm500365s
2176 9757 58 None -831 8 Human 8.1 pEC50 = 8.1 Binding
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
ChEMBL None None None None 10.1021/jm500365s
439302 9757 58 None -831 8 Human 8.1 pEC50 = 8.1 Binding
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
ChEMBL None None None None 10.1021/jm500365s
CHEMBL395429 9757 58 None -831 8 Human 8.1 pEC50 = 8.1 Binding
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
ChEMBL None None None None 10.1021/jm500365s
DB00107 9757 58 None -831 8 Human 8.1 pEC50 = 8.1 Binding
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
ChEMBL None None None None 10.1021/jm500365s
10411308 208013 0 None 2 3 Human 8.1 pEC50 = 8.1 Binding
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
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm901084f
CHEMBL603708 208013 0 None 2 3 Human 8.1 pEC50 = 8.1 Binding
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
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm901084f
118720264 122615 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354575 122615 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
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
ChEMBL 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 10.1021/jm500365s
118720280 122630 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354590 122630 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
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
ChEMBL 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 10.1021/jm500365s
118720271 122621 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354581 122621 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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
ChEMBL 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 10.1021/jm500365s
118720290 122642 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354602 122642 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
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
ChEMBL 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 10.1021/jm500365s
118719827 122529 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353938 122529 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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
ChEMBL 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 10.1021/jm500365s
118719838 122540 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353949 122540 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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
ChEMBL 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 10.1021/jm500365s
118719831 122533 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353942 122533 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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
ChEMBL 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 10.1021/jm500365s
118719837 122539 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353948 122539 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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
ChEMBL 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 10.1021/jm500365s
118719836 122538 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353947 122538 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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
ChEMBL 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 10.1021/jm500365s
135413563 129708 25 None - 2 Human 6.1 pEC50 = 6.1 Binding
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
ChEMBL 600 4 2 7 4.3 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1021/jm901084f
CHEMBL360648 129708 25 None - 2 Human 6.1 pEC50 = 6.1 Binding
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
ChEMBL 600 4 2 7 4.3 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1021/jm901084f
135413563 129708 25 None - 2 Human 6.1 pEC50 = 6.1 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 600 4 2 7 4.3 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1016/j.bmcl.2004.04.107
CHEMBL360648 129708 25 None - 2 Human 6.1 pEC50 = 6.1 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 600 4 2 7 4.3 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1016/j.bmcl.2004.04.107
118720260 122611 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3354571 122611 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
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
ChEMBL 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 10.1021/jm500365s
10187625 134068 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 553 4 1 5 4.7 Cc1cc(C(=O)N2CCCCc3sccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1016/j.bmcl.2004.04.107
CHEMBL365862 134068 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 553 4 1 5 4.7 Cc1cc(C(=O)N2CCCCc3sccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1016/j.bmcl.2004.04.107
118719819 122521 0 None - 0 Human 8.0 pEC50 = 8 Binding
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
ChEMBL 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 10.1021/jm500365s
CHEMBL3353930 122521 0 None - 0 Human 8.0 pEC50 = 8 Binding
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
ChEMBL 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 10.1021/jm500365s
44332239 11305 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
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
ChEMBL 466 4 1 3 6.3 COc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.02.103
CHEMBL102311 11305 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
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
ChEMBL 466 4 1 3 6.3 COc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.02.103
172997 9112 57 None - 2 Rat 9.3 pIC50 = 9.3 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(99)00279-6
2238 9112 57 None - 2 Rat 9.3 pIC50 = 9.3 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(99)00279-6
CHEMBL49429 9112 57 None - 2 Rat 9.3 pIC50 = 9.3 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(99)00279-6
DB06666 9112 57 None - 2 Rat 9.3 pIC50 = 9.3 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(99)00279-6
10648029 112197 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
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
ChEMBL 469 3 1 3 6.2 Cc1cccc(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)c1C 10.1021/jm980179c
CHEMBL311931 112197 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
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
ChEMBL 469 3 1 3 6.2 Cc1cccc(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)c1C 10.1021/jm980179c
10743786 170258 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
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
ChEMBL 493 3 1 3 6.4 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccc(F)cc1Cl 10.1021/jm980179c
CHEMBL420031 170258 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
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
ChEMBL 493 3 1 3 6.4 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccc(F)cc1Cl 10.1021/jm980179c
15308000 194123 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
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)
ChEMBL 438 3 1 3 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)cc1 10.1016/s0960-894x(99)00278-4
CHEMBL49322 194123 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
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)
ChEMBL 438 3 1 3 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)cc1 10.1016/s0960-894x(99)00278-4
9826033 64236 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity towards V2 receptorBinding affinity towards V2 receptor
ChEMBL 471 4 2 2 6.7 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL165670 64236 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity towards V2 receptorBinding affinity towards V2 receptor
ChEMBL 471 4 2 2 6.7 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
56848490 153530 0 None - 0 Human 9.0 pIC50 = 9 Binding
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.
ChEMBL 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 nan
CHEMBL3924331 153530 0 None - 0 Human 9.0 pIC50 = 9 Binding
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.
ChEMBL 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 nan
44213443 183797 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 440 3 1 4 4.8 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
CHEMBL46295 183797 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 440 3 1 4 4.8 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
10742418 111263 0 None - 0 Human 9.0 pIC50 = 9 Binding
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
ChEMBL 455 3 1 3 5.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/jm980179c
CHEMBL310416 111263 0 None - 0 Human 9.0 pIC50 = 9 Binding
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
ChEMBL 455 3 1 3 5.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/jm980179c
172997 9112 57 None 64 2 Human 9.0 pIC50 = 9 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2005.08.007
2238 9112 57 None 64 2 Human 9.0 pIC50 = 9 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2005.08.007
CHEMBL49429 9112 57 None 64 2 Human 9.0 pIC50 = 9 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2005.08.007
DB06666 9112 57 None 64 2 Human 9.0 pIC50 = 9 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2005.08.007
11490613 168517 0 None - 0 Rat 9.0 pIC50 = 9 Binding
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
ChEMBL 636 9 1 6 6.6 CN1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL413748 168517 0 None - 0 Rat 9.0 pIC50 = 9 Binding
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
ChEMBL 636 9 1 6 6.6 CN1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
11490514 137467 0 None - 0 Human 9.0 pIC50 = 9 Binding
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
ChEMBL 622 10 1 6 7.1 CN1CCN(CCCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL368354 137467 0 None - 0 Human 9.0 pIC50 = 9 Binding
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
ChEMBL 622 10 1 6 7.1 CN1CCN(CCCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
44213442 108807 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 460 3 1 4 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccc(F)cc1Cl 10.1016/s0960-894x(99)00279-6
CHEMBL301788 108807 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 460 3 1 4 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccc(F)cc1Cl 10.1016/s0960-894x(99)00279-6
21467141 126445 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 486 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
CHEMBL347020 126445 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 486 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
172997 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1021/jm980179c
2238 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1021/jm980179c
CHEMBL49429 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1021/jm980179c
DB06666 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1021/jm980179c
172997 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.08.053
2238 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.08.053
CHEMBL49429 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.08.053
DB06666 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.08.053
172997 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00095-0
2238 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00095-0
CHEMBL49429 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00095-0
DB06666 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00095-0
172997 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00084-6
2238 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00084-6
CHEMBL49429 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00084-6
DB06666 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00084-6
172997 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
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)
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(99)00278-4
2238 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
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)
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(99)00278-4
CHEMBL49429 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
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)
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(99)00278-4
DB06666 9112 57 None 64 2 Human 8.9 pIC50 = 8.9 Binding
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)
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(99)00278-4
44378719 64192 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
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
ChEMBL 629 6 1 5 7.0 CN1CCN(Cc2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1 10.1016/s0960-894x(00)00095-0
CHEMBL165340 64192 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
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
ChEMBL 629 6 1 5 7.0 CN1CCN(Cc2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1 10.1016/s0960-894x(00)00095-0
89701036 158582 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
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.
ChEMBL 496 7 2 7 3.2 O=c1n(Cc2nnc(Cc3ccccc3F)[nH]2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3965167 158582 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
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.
ChEMBL 496 7 2 7 3.2 O=c1n(Cc2nnc(Cc3ccccc3F)[nH]2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
10459252 59425 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 517 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
CHEMBL159359 59425 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 517 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
69940391 155328 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
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.
ChEMBL 512 7 2 7 3.7 O=c1n(Cc2nnc(Cc3ccccc3Cl)[nH]2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3938717 155328 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
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.
ChEMBL 512 7 2 7 3.7 O=c1n(Cc2nnc(Cc3ccccc3Cl)[nH]2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
10003306 210552 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
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
ChEMBL 439 3 1 3 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
CHEMBL68085 210552 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
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
ChEMBL 439 3 1 3 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
10003306 210552 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
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.
ChEMBL 439 3 1 3 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL68085 210552 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
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.
ChEMBL 439 3 1 3 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
18917497 108497 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 486 3 1 4 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1Br 10.1016/s0960-894x(99)00279-6
CHEMBL299532 108497 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 486 3 1 4 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1Br 10.1016/s0960-894x(99)00279-6
10098338 126881 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 524 4 2 4 6.9 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
CHEMBL350973 126881 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 524 4 2 4 6.9 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
44213444 108691 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 442 3 1 4 5.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1Cl 10.1016/s0960-894x(99)00279-6
CHEMBL300963 108691 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 442 3 1 4 5.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1Cl 10.1016/s0960-894x(99)00279-6
10672170 212175 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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
ChEMBL 473 3 1 3 6.1 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/jm980179c
CHEMBL80029 212175 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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
ChEMBL 473 3 1 3 6.1 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/jm980179c
10696913 212348 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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
ChEMBL 505 4 1 4 6.3 COc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1NC(=O)c1ccc(Cl)cc1Cl 10.1021/jm980179c
CHEMBL81269 212348 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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
ChEMBL 505 4 1 4 6.3 COc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1NC(=O)c1ccc(Cl)cc1Cl 10.1021/jm980179c
44336418 114964 0 None - 0 Human 8.0 pIC50 = 8 Binding
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
ChEMBL 569 6 2 5 5.0 COC(=O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3C)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL319636 114964 0 None - 0 Human 8.0 pIC50 = 8 Binding
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
ChEMBL 569 6 2 5 5.0 COC(=O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3C)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
56848557 153451 0 None - 0 Human 8.0 pIC50 = 8 Binding
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.
ChEMBL 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 nan
CHEMBL3923775 153451 0 None - 0 Human 8.0 pIC50 = 8 Binding
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.
ChEMBL 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 nan
44335345 11943 0 None 4 2 Human 8.0 pIC50 = 8 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 505 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(02)00649-2
CHEMBL105961 11943 0 None 4 2 Human 8.0 pIC50 = 8 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 505 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(02)00649-2
11386922 67214 0 None - 0 Rat 8.0 pIC50 = 8 Binding
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
ChEMBL 525 6 1 5 6.7 COc1cc(C(=O)N2CCCC(N(C)C)c3sccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL175212 67214 0 None - 0 Rat 8.0 pIC50 = 8 Binding
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
ChEMBL 525 6 1 5 6.7 COc1cc(C(=O)N2CCCC(N(C)C)c3sccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm030287l
11272841 67574 0 None - 0 Rat 8.0 pIC50 = 8 Binding
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
ChEMBL 550 7 1 5 6.6 O=C(Nc1ccc(C(=O)N2CCCN(CCN3CCCC3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL176146 67574 0 None - 0 Rat 8.0 pIC50 = 8 Binding
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
ChEMBL 550 7 1 5 6.6 O=C(Nc1ccc(C(=O)N2CCCN(CCN3CCCC3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
10840974 68553 0 None - 0 Rat 8.0 pIC50 = 8 Binding
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
ChEMBL 579 7 1 6 5.8 CN1CCN(CCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccsc32)CC1 10.1021/jm030287l
CHEMBL177285 68553 0 None - 0 Rat 8.0 pIC50 = 8 Binding
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
ChEMBL 579 7 1 6 5.8 CN1CCN(CCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccsc32)CC1 10.1021/jm030287l
11763684 138135 0 None - 0 Human 8.0 pIC50 = 8 Binding
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
ChEMBL 650 9 1 6 7.0 CN1CCCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL368818 138135 0 None - 0 Human 8.0 pIC50 = 8 Binding
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
ChEMBL 650 9 1 6 7.0 CN1CCCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
11798757 211067 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 475 3 1 3 6.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1C(F)(F)F 10.1021/jm980179c
CHEMBL71305 211067 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 475 3 1 3 6.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1C(F)(F)F 10.1021/jm980179c
44352767 121899 0 None - 0 Human 7.0 pIC50 = 7 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 528 6 1 3 7.8 O=C(Nc1ccc(C(=O)N2CCC(CC(F)F)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
CHEMBL334363 121899 0 None - 0 Human 7.0 pIC50 = 7 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 528 6 1 3 7.8 O=C(Nc1ccc(C(=O)N2CCC(CC(F)F)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
69940642 158558 0 None - 0 Human 7.0 pIC50 = 7 Binding
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.
ChEMBL 509 6 1 7 4.4 O=c1n(Cc2ccnc(-c3ccccc3Cl)n2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3964983 158558 0 None - 0 Human 7.0 pIC50 = 7 Binding
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.
ChEMBL 509 6 1 7 4.4 O=c1n(Cc2ccnc(-c3ccccc3Cl)n2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
10603742 135450 0 None - 0 Rat 7.0 pIC50 = 7 Binding
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
ChEMBL 607 6 1 6 5.7 CN1CCCN(CC(=O)N2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccsc32)CC1 10.1021/jm030287l
CHEMBL366816 135450 0 None - 0 Rat 7.0 pIC50 = 7 Binding
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
ChEMBL 607 6 1 6 5.7 CN1CCCN(CC(=O)N2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccsc32)CC1 10.1021/jm030287l
44386548 139133 0 None - 0 Rat 7.0 pIC50 = 7 Binding
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
ChEMBL 433 4 1 4 5.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)C)c3sccc32)cc1 10.1021/jm00137a004
CHEMBL369712 139133 0 None - 0 Rat 7.0 pIC50 = 7 Binding
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
ChEMBL 433 4 1 4 5.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)C)c3sccc32)cc1 10.1021/jm00137a004
10527137 19559 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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
ChEMBL 441 4 0 3 5.3 Cc1ccccc1C(=O)N(C)c1ccc(C(=O)N2CCCC(N(C)C)c3ccccc32)cc1 10.1021/jm960133o
CHEMBL118805 19559 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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
ChEMBL 441 4 0 3 5.3 Cc1ccccc1C(=O)N(C)c1ccc(C(=O)N2CCCC(N(C)C)c3ccccc32)cc1 10.1021/jm960133o
10499401 20804 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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
ChEMBL 370 4 1 2 4.5 O=C(Cc1ccccc1)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL119730 20804 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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
ChEMBL 370 4 1 2 4.5 O=C(Cc1ccccc1)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
44433372 96701 0 None - 0 Human 6.0 pIC50 = 6 Binding
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
ChEMBL 426 5 3 3 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)Nc2ccccc2C(=O)O)c(Cl)c1 10.1016/j.bmcl.2007.08.053
CHEMBL237987 96701 0 None - 0 Human 6.0 pIC50 = 6 Binding
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
ChEMBL 426 5 3 3 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)Nc2ccccc2C(=O)O)c(Cl)c1 10.1016/j.bmcl.2007.08.053
44433375 96962 0 None - 0 Human 6.0 pIC50 = 6 Binding
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
ChEMBL 505 7 3 4 5.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)Nc2ccccc2Cn2cccc2C(=O)O)c(Cl)c1 10.1016/j.bmcl.2007.08.053
CHEMBL238206 96962 0 None - 0 Human 6.0 pIC50 = 6 Binding
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
ChEMBL 505 7 3 4 5.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)Nc2ccccc2Cn2cccc2C(=O)O)c(Cl)c1 10.1016/j.bmcl.2007.08.053
10710850 126025 0 None - 0 Human 6.0 pIC50 = 6 Binding
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
ChEMBL 320 2 0 2 4.3 O=C(c1ccc(N2CCCC2)cc1)N1CCCCc2ccccc21 10.1021/jm000108p
CHEMBL343538 126025 0 None - 0 Human 6.0 pIC50 = 6 Binding
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
ChEMBL 320 2 0 2 4.3 O=C(c1ccc(N2CCCC2)cc1)N1CCCCc2ccccc21 10.1021/jm000108p
11756081 25671 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL128398 25671 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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
ChEMBL 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 10.1021/jm00077a002
10098227 25729 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL128680 25729 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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
ChEMBL 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 10.1021/jm00077a002
9983763 26156 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL129234 26156 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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
ChEMBL 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 10.1021/jm00077a002
10436744 27941 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL131269 27941 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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
ChEMBL 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 10.1021/jm00077a002
10256140 28290 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL131613 28290 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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
ChEMBL 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 10.1021/jm00077a002
44352440 123549 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL337667 123549 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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
ChEMBL 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 10.1021/jm00077a002
44352497 123835 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL339151 123835 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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
ChEMBL 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 10.1021/jm00077a002
10324129 175331 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL435613 175331 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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
ChEMBL 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 10.1021/jm00077a002
10432863 105092 0 None - 0 Rat 4.0 pIC50 = 4 Binding
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
ChEMBL 430 4 2 4 2.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@](O)(CN)C2 10.1021/jm00077a002
CHEMBL274955 105092 0 None - 0 Rat 4.0 pIC50 = 4 Binding
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
ChEMBL 430 4 2 4 2.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@](O)(CN)C2 10.1021/jm00077a002
CHEMBL2332718 216314 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
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
ChEMBL 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 10.1016/j.bmcl.2012.12.041
10461417 114078 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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
ChEMBL 612 8 2 4 6.6 CN(C)CCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL317243 114078 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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
ChEMBL 612 8 2 4 6.6 CN(C)CCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
44336636 170944 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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
ChEMBL 585 7 3 4 6.0 O=C(NCCO)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL421039 170944 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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
ChEMBL 585 7 3 4 6.0 O=C(NCCO)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
67409933 156844 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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.
ChEMBL 554 8 1 7 5.5 COc1ccc(Cn2c(-c3ccc(Cl)cc3)nn(Cc3nnc(Cc4c(Cl)cccc4Cl)[nH]3)c2=O)cc1 nan
CHEMBL3950716 156844 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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.
ChEMBL 554 8 1 7 5.5 COc1ccc(Cn2c(-c3ccc(Cl)cc3)nn(Cc3nnc(Cc4c(Cl)cccc4Cl)[nH]3)c2=O)cc1 nan
56848553 152395 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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.
ChEMBL 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 nan
CHEMBL3915616 152395 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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.
ChEMBL 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 nan
9869993 172331 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 485 4 2 2 7.0 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3CCCc4c[nH]c5cccc3c45)cc2)cc1 10.1016/s0960-894x(02)01059-4
CHEMBL424183 172331 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 485 4 2 2 7.0 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3CCCc4c[nH]c5cccc3c45)cc2)cc1 10.1016/s0960-894x(02)01059-4
44433363 153430 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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
ChEMBL 489 3 1 3 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2C=C3CCC(=O)N3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2007.08.053
CHEMBL392363 153430 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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
ChEMBL 489 3 1 3 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2C=C3CCC(=O)N3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2007.08.053
9961036 18498 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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
ChEMBL 643 5 1 5 6.7 CN1CCN(C(=O)c2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1 10.1016/s0960-894x(00)00095-0
CHEMBL1181319 18498 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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
ChEMBL 643 5 1 5 6.7 CN1CCN(C(=O)c2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1 10.1016/s0960-894x(00)00095-0
CHEMBL164387 18498 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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
ChEMBL 643 5 1 5 6.7 CN1CCN(C(=O)c2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1 10.1016/s0960-894x(00)00095-0
53378729 149233 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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.
ChEMBL 473 7 0 6 5.2 C=CCn1c(-c2ccc(Cl)cc2)nn(Cc2cncn2Cc2c(Cl)cccc2Cl)c1=O nan
CHEMBL3890193 149233 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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.
ChEMBL 473 7 0 6 5.2 C=CCn1c(-c2ccc(Cl)cc2)nn(Cc2cncn2Cc2c(Cl)cccc2Cl)c1=O nan
10620180 120281 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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
ChEMBL 386 3 1 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCOc3ccccc32)cc1 10.1021/jm960133o
CHEMBL332060 120281 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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
ChEMBL 386 3 1 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCOc3ccccc32)cc1 10.1021/jm960133o
23598597 100872 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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
ChEMBL 528 5 2 4 5.8 COc1cc(NC(=O)c2cc(F)ccc2C)ccc1C(=O)N1CCC2(C=C(C(=O)O)CC2)Cc2ccccc21 10.1016/j.bmcl.2007.09.059
CHEMBL249133 100872 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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
ChEMBL 528 5 2 4 5.8 COc1cc(NC(=O)c2cc(F)ccc2C)ccc1C(=O)N1CCC2(C=C(C(=O)O)CC2)Cc2ccccc21 10.1016/j.bmcl.2007.09.059
CHEMBL338018 218381 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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.
ChEMBL 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 10.1021/jm00099a019
69940703 152977 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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.
ChEMBL 490 6 0 6 5.8 O=c1n(Cc2ncc(Cc3cccc(C(F)(F)F)c3)s2)nc(-c2ccc(Cl)cc2)n1C1CC1 nan
CHEMBL3920097 152977 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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.
ChEMBL 490 6 0 6 5.8 O=c1n(Cc2ncc(Cc3cccc(C(F)(F)F)c3)s2)nc(-c2ccc(Cl)cc2)n1C1CC1 nan
CHEMBL2112248 216014 0 None - 2 Rat 6.0 pIC50 = 6.0 Binding
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.
ChEMBL 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 10.1021/jm00099a019
44273368 105570 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
CHEMBL278377 105570 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
10031372 25648 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL128258 25648 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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
ChEMBL 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 10.1021/jm00077a002
44352433 124053 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL339498 124053 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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
ChEMBL 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 10.1021/jm00077a002
9881053 127023 0 None - 1 Pig 5.0 pIC50 = 5.0 Binding
Ability to displace [3H]AVP from Vasopressin V2 receptorAbility to displace [3H]AVP from Vasopressin V2 receptor
ChEMBL 339 5 1 4 4.1 CCCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
CHEMBL35226 127023 0 None - 1 Pig 5.0 pIC50 = 5.0 Binding
Ability to displace [3H]AVP from Vasopressin V2 receptorAbility to displace [3H]AVP from Vasopressin V2 receptor
ChEMBL 339 5 1 4 4.1 CCCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
CHEMBL129733 215461 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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.
ChEMBL 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 10.1021/jm00099a019
CHEMBL338020 218382 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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.
ChEMBL 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 10.1021/jm00099a019
10030575 28891 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL132210 28891 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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
ChEMBL 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 10.1021/jm00077a002
44273077 105960 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
CHEMBL281361 105960 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
3793 209988 77 None - 1 Human 4.9 pIC50 = 4.9 Binding
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
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 209988 77 None - 1 Human 4.9 pIC50 = 4.9 Binding
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
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 209988 77 None - 1 Human 4.9 pIC50 = 4.9 Binding
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
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
44352777 28154 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 572 7 2 5 6.4 O=C(Nc1ccc(C(=O)N2CCC(CCS(=O)(=O)O)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
CHEMBL131439 28154 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 572 7 2 5 6.4 O=C(Nc1ccc(C(=O)N2CCC(CCS(=O)(=O)O)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
53378841 152675 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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.
ChEMBL 508 6 1 6 5.1 O=c1n(Cc2cncc(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1CC(O)C(F)(F)F nan
CHEMBL3917760 152675 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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.
ChEMBL 508 6 1 6 5.1 O=c1n(Cc2cncc(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1CC(O)C(F)(F)F nan
53378731 160507 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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.
ChEMBL 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 nan
CHEMBL3981686 160507 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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.
ChEMBL 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 nan
119369 9384 74 None -1 8 Rat 7.9 pIC50 = 7.9 Binding
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
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm960133o
2197 9384 74 None -1 8 Rat 7.9 pIC50 = 7.9 Binding
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
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm960133o
4004 9384 74 None -1 8 Rat 7.9 pIC50 = 7.9 Binding
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
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm960133o
CHEMBL420762 9384 74 None -1 8 Rat 7.9 pIC50 = 7.9 Binding
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
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm960133o
44377961 64288 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 585 5 3 4 6.6 O=C(Nc1ccc(C(=O)N2CCCc3c(S(=O)(=O)O)[nH]c4cccc2c34)cc1Cl)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL166135 64288 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 585 5 3 4 6.6 O=C(Nc1ccc(C(=O)N2CCCc3c(S(=O)(=O)O)[nH]c4cccc2c34)cc1Cl)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
19699093 126816 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 428 3 2 4 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
CHEMBL350383 126816 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 428 3 2 4 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
10595255 33312 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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
ChEMBL 368 2 0 2 5.3 O=C(c1ccc(N2CCCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
CHEMBL136065 33312 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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
ChEMBL 368 2 0 2 5.3 O=C(c1ccc(N2CCCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
56848685 158574 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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.
ChEMBL 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 nan
CHEMBL3965109 158574 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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.
ChEMBL 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 nan
10810069 18495 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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
ChEMBL 384 3 1 2 5.1 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)cc1C 10.1021/jm960133o
CHEMBL118128 18495 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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
ChEMBL 384 3 1 2 5.1 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)cc1C 10.1021/jm960133o
CHEMBL2370623 216670 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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.
ChEMBL 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 10.1021/jm00099a019
10391259 25668 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL128388 25668 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
10052640 27899 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL131239 27899 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
10483039 85272 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL2111851 85272 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
44433360 96224 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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
ChEMBL 418 2 0 4 4.5 Cc1ccn(-c2ccc(C(=O)N3C=C4CCC(=O)N4Cc4ccccc43)c(Cl)c2)n1 10.1016/j.bmcl.2007.08.053
CHEMBL237120 96224 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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
ChEMBL 418 2 0 4 4.5 Cc1ccn(-c2ccc(C(=O)N3C=C4CCC(=O)N4Cc4ccccc43)c(Cl)c2)n1 10.1016/j.bmcl.2007.08.053
3793 209988 77 None - 1 Human 4.9 pIC50 = 4.9 Binding
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
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 209988 77 None - 1 Human 4.9 pIC50 = 4.9 Binding
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
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 209988 77 None - 1 Human 4.9 pIC50 = 4.9 Binding
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
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
88064173 158405 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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.
ChEMBL 530 7 1 6 5.4 O=c1n(Cc2nnc(Cc3c(Cl)cccc3Cl)[nH]2)nc(-c2ccc(Cl)cc2)n1CCC(F)(F)F nan
CHEMBL3963751 158405 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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.
ChEMBL 530 7 1 6 5.4 O=c1n(Cc2nnc(Cc3c(Cl)cccc3Cl)[nH]2)nc(-c2ccc(Cl)cc2)n1CCC(F)(F)F nan
56848556 153815 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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.
ChEMBL 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 nan
CHEMBL3926829 153815 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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.
ChEMBL 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 nan
10838493 20686 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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
ChEMBL 481 4 1 3 6.3 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccc(Cl)cc3Cl)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL119638 20686 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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
ChEMBL 481 4 1 3 6.3 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccc(Cl)cc3Cl)cc2)c2ccccc21 10.1021/jm960133o
10742994 117156 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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
ChEMBL 470 6 2 4 4.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)CC(N)=O)c3ccccc32)cc1 10.1021/jm960133o
CHEMBL324251 117156 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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
ChEMBL 470 6 2 4 4.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)CC(N)=O)c3ccccc32)cc1 10.1021/jm960133o
9850567 64224 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 551 5 3 4 5.9 O=C(Nc1ccc(C(=O)N2CCCc3c(S(=O)(=O)O)[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL165554 64224 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 551 5 3 4 5.9 O=C(Nc1ccc(C(=O)N2CCCc3c(S(=O)(=O)O)[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
21837162 109310 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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.
ChEMBL 453 4 1 4 5.7 CSc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL304060 109310 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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.
ChEMBL 453 4 1 4 5.7 CSc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
10503021 109513 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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.
ChEMBL 435 3 1 3 5.6 Cc1cccc(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)c1C 10.1016/s0960-894x(03)00388-3
CHEMBL304956 109513 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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.
ChEMBL 435 3 1 3 5.6 Cc1cccc(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)c1C 10.1016/s0960-894x(03)00388-3
10570880 33363 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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
ChEMBL 365 2 0 3 4.8 Cc1ccn(-c2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1 10.1021/jm000108p
CHEMBL136109 33363 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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
ChEMBL 365 2 0 3 4.8 Cc1ccn(-c2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1 10.1021/jm000108p
10498917 122788 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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
ChEMBL 362 2 0 2 5.0 CN(C)c1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL335592 122788 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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
ChEMBL 362 2 0 2 5.0 CN(C)c1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(Cl)c1 10.1021/jm000108p
44335343 114247 0 None 1 2 Human 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 519 3 1 3 6.6 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(CC4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(02)00649-2
CHEMBL318392 114247 0 None 1 2 Human 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 519 3 1 3 6.6 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(CC4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(02)00649-2
14981580 85646 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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
ChEMBL 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 10.1021/jm00031a004
CHEMBL2112895 85646 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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
ChEMBL 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 10.1021/jm00031a004
19699093 126816 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 428 3 2 4 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
CHEMBL350383 126816 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 428 3 2 4 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
CHEMBL2112247 216013 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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.
ChEMBL 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 10.1021/jm00099a019
9805972 105391 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
CHEMBL276990 105391 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
44273346 169726 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
CHEMBL417458 169726 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
44352492 25742 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL128749 25742 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
44352150 25637 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL128194 25637 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
10413998 25820 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL128879 25820 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
44352299 123581 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 416 3 1 4 4.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)/C(=N\O)C2 10.1021/jm00077a002
CHEMBL337842 123581 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 416 3 1 4 4.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)/C(=N\O)C2 10.1021/jm00077a002
10347314 123705 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL338499 123705 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
10459672 124269 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL340016 124269 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
10574499 119765 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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
ChEMBL 427 4 1 3 5.3 Cc1cccc(C(=O)Nc2ccc(C(=O)N3CCCC(N(C)C)c4ccccc43)cc2)c1 10.1021/jm960133o
CHEMBL331098 119765 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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
ChEMBL 427 4 1 3 5.3 Cc1cccc(C(=O)Nc2ccc(C(=O)N3CCCC(N(C)C)c4ccccc43)cc2)c1 10.1021/jm960133o
10524974 120837 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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
ChEMBL 399 3 1 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(C)c3ccccc32)cc1 10.1021/jm960133o
CHEMBL332685 120837 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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
ChEMBL 399 3 1 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(C)c3ccccc32)cc1 10.1021/jm960133o
10984131 126821 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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
ChEMBL 517 4 2 4 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3ccc(C(=O)O)n3Cc3ccccc32)c(Cl)c1 10.1016/s0960-894x(00)00095-0
CHEMBL350408 126821 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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
ChEMBL 517 4 2 4 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3ccc(C(=O)O)n3Cc3ccccc32)c(Cl)c1 10.1016/s0960-894x(00)00095-0
10789117 211391 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 437 4 1 4 5.0 COc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
CHEMBL73286 211391 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 437 4 1 4 5.0 COc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
23598595 161582 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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
ChEMBL 542 5 2 3 7.0 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
CHEMBL400266 161582 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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
ChEMBL 542 5 2 3 7.0 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
21837107 210679 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1cc(Cl)ccc1Cl 10.1016/s0960-894x(03)00388-3
CHEMBL68948 210679 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1cc(Cl)ccc1Cl 10.1016/s0960-894x(03)00388-3
10789117 211391 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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.
ChEMBL 437 4 1 4 5.0 COc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL73286 211391 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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.
ChEMBL 437 4 1 4 5.0 COc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
44378886 63453 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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
ChEMBL 556 6 2 5 6.4 CN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1O)C2 10.1016/s0960-894x(00)00095-0
CHEMBL164226 63453 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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
ChEMBL 556 6 2 5 6.4 CN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1O)C2 10.1016/s0960-894x(00)00095-0
10601045 20733 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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
ChEMBL 487 4 1 3 6.6 O=C(Nc1ccc(C(=O)N2CCCC(N3CCCCC3)c3ccccc32)cc1)c1ccccc1Cl 10.1021/jm960133o
CHEMBL119671 20733 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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
ChEMBL 487 4 1 3 6.6 O=C(Nc1ccc(C(=O)N2CCCC(N3CCCCC3)c3ccccc32)cc1)c1ccccc1Cl 10.1021/jm960133o
19699060 62921 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 466 3 2 4 5.4 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1)c1ccc(F)cc1Cl 10.1016/s0960-894x(00)00084-6
CHEMBL162588 62921 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 466 3 2 4 5.4 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1)c1ccc(F)cc1Cl 10.1016/s0960-894x(00)00084-6
10690528 120288 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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
ChEMBL 370 3 1 2 4.8 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)cc1 10.1021/jm960133o
CHEMBL332090 120288 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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
ChEMBL 370 3 1 2 4.8 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)cc1 10.1021/jm960133o
CHEMBL338294 218385 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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.
ChEMBL 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 10.1021/jm00099a019
10347928 125244 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL341289 125244 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
44352165 125332 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL341507 125332 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
10324995 171112 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL421248 171112 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
ChEMBL 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 10.1021/jm00077a002
44352804 25731 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 536 7 2 4 7.0 O=C(O)CC[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL128688 25731 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 536 7 2 4 7.0 O=C(O)CC[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
56848624 167546 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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.
ChEMBL 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 nan
CHEMBL4114132 167546 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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.
ChEMBL 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 nan
44377903 64075 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 505 4 2 2 7.3 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1Cl)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL165076 64075 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 505 4 2 2 7.3 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1Cl)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
44310163 109000 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1c(Cl)cccc1Cl 10.1016/s0960-894x(03)00388-3
CHEMBL302955 109000 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1c(Cl)cccc1Cl 10.1016/s0960-894x(03)00388-3
11757222 114779 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 547 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2C[C@H]3C4CCC(C4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
CHEMBL319418 114779 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 547 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2C[C@H]3C4CCC(C4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
10043741 124959 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity against Vasopressin V2 receptor was determined in Brattleboro ratsBinding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm020133q
CHEMBL340893 124959 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity against Vasopressin V2 receptor was determined in Brattleboro ratsBinding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm020133q
10043741 124959 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity towards rat Vasopressin V2 receptorBinding affinity towards rat Vasopressin V2 receptor
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
CHEMBL340893 124959 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity towards rat Vasopressin V2 receptorBinding affinity towards rat Vasopressin V2 receptor
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
86690916 157704 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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.
ChEMBL 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 nan
CHEMBL3957738 157704 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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.
ChEMBL 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 nan
10527129 20621 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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
ChEMBL 441 4 2 3 4.9 CC(=O)NC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL119591 20621 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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
ChEMBL 441 4 2 3 4.9 CC(=O)NC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
19699133 126709 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 496 3 1 5 5.9 Cn1cc2c(n1)-c1sccc1N(C(=O)c1ccc(NC(=O)c3ccc(Cl)cc3Cl)cc1)CC2 10.1016/s0960-894x(00)00084-6
CHEMBL349506 126709 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 496 3 1 5 5.9 Cn1cc2c(n1)-c1sccc1N(C(=O)c1ccc(NC(=O)c3ccc(Cl)cc3Cl)cc1)CC2 10.1016/s0960-894x(00)00084-6
CHEMBL340204 218411 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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.
ChEMBL 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 10.1021/jm00099a019
44272990 106382 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
CHEMBL283994 106382 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
44352481 123799 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL338951 123799 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
10347928 125244 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL341289 125244 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
22405325 140338 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 427 4 0 4 5.5 CN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(-c3cccs3)cc1)C2 10.1016/j.bmcl.2005.08.007
CHEMBL371055 140338 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 427 4 0 4 5.5 CN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(-c3cccs3)cc1)C2 10.1016/j.bmcl.2005.08.007
10098755 28258 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL131581 28258 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
9985844 123426 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL336992 123426 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
2812 11551 101 None - 34 Human 4.8 pIC50 = 4.8 Binding
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
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
CHEMBL104 11551 101 None - 34 Human 4.8 pIC50 = 4.8 Binding
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
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
5280343 195054 124 None -147 31 Human 4.8 pIC50 = 4.8 Binding
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
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL1520590 195054 124 None -147 31 Human 4.8 pIC50 = 4.8 Binding
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
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 195054 124 None -147 31 Human 4.8 pIC50 = 4.8 Binding
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
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
5280343 195054 124 None -147 31 Human 4.8 pIC50 = 4.8 Binding
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
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL1520590 195054 124 None -147 31 Human 4.8 pIC50 = 4.8 Binding
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
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 195054 124 None -147 31 Human 4.8 pIC50 = 4.8 Binding
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
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
2812 11551 101 None - 34 Human 4.8 pIC50 = 4.8 Binding
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
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
CHEMBL104 11551 101 None - 34 Human 4.8 pIC50 = 4.8 Binding
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
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
44332208 11017 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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
ChEMBL 504 3 1 2 7.6 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.02.103
CHEMBL100447 11017 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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
ChEMBL 504 3 1 2 7.6 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.02.103
44352768 122034 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 536 7 2 4 7.0 O=C(O)CC[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL334777 122034 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 536 7 2 4 7.0 O=C(O)CC[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
44336784 115985 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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
ChEMBL 626 9 2 4 7.0 CN(C)CCCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL321656 115985 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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
ChEMBL 626 9 2 4 7.0 CN(C)CCCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
56849411 159957 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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.
ChEMBL 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 nan
CHEMBL3976964 159957 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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.
ChEMBL 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 nan
10528416 111506 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 471 4 1 4 5.6 COc1cc(Cl)ccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
CHEMBL310581 111506 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 471 4 1 4 5.6 COc1cc(Cl)ccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
10691737 33960 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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
ChEMBL 388 2 0 2 5.6 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2cc(Cl)ccc21 10.1021/jm000108p
CHEMBL136628 33960 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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
ChEMBL 388 2 0 2 5.6 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2cc(Cl)ccc21 10.1021/jm000108p
18917508 194862 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 453 4 1 6 4.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1[N+](=O)[O-] 10.1016/s0960-894x(99)00279-6
CHEMBL49796 194862 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 453 4 1 6 4.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1[N+](=O)[O-] 10.1016/s0960-894x(99)00279-6
14981581 85644 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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
ChEMBL 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 10.1021/jm00031a004
CHEMBL2112893 85644 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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
ChEMBL 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 10.1021/jm00031a004
10763869 18647 1 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 406 4 1 3 4.5 O=C(c1ccc(NS(=O)(=O)c2ccccc2)cc1)N1CCCCc2ccccc21 10.1021/jm960133o
CHEMBL118244 18647 1 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 406 4 1 3 4.5 O=C(c1ccc(NS(=O)(=O)c2ccccc2)cc1)N1CCCCc2ccccc21 10.1021/jm960133o
CHEMBL338308 218387 0 None - 2 Rat 5.8 pIC50 = 5.8 Binding
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.
ChEMBL 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 10.1021/jm00099a019
44352141 28222 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL131538 28222 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
10323684 123823 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL339096 123823 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
44273080 105395 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
CHEMBL277022 105395 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
10834761 121316 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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
ChEMBL 399 3 1 3 4.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCN(C)Cc3ccccc32)cc1 10.1021/jm960133o
CHEMBL333652 121316 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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
ChEMBL 399 3 1 3 4.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCN(C)Cc3ccccc32)cc1 10.1021/jm960133o
23505561 126769 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 527 4 1 4 7.1 CC(=O)n1cc2c3c(cccc31)N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccc(C)cc3)cc1)CCC2 10.1016/s0960-894x(02)01059-4
CHEMBL349965 126769 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 527 4 1 4 7.1 CC(=O)n1cc2c3c(cccc31)N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccc(C)cc3)cc1)CCC2 10.1016/s0960-894x(02)01059-4
67412584 157556 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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.
ChEMBL 473 6 1 5 5.1 O=c1n(Cc2ncc(Cc3cccc(C(F)(F)F)c3)[nH]2)nc(-c2ccc(Cl)cc2)n1C1CC1 nan
CHEMBL3956553 157556 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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.
ChEMBL 473 6 1 5 5.1 O=c1n(Cc2ncc(Cc3cccc(C(F)(F)F)c3)[nH]2)nc(-c2ccc(Cl)cc2)n1C1CC1 nan
10832492 121577 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 362 3 1 3 4.6 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccsc1 10.1021/jm960133o
CHEMBL334009 121577 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 362 3 1 3 4.6 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccsc1 10.1021/jm960133o
44309805 211061 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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.
ChEMBL 434 3 1 3 6.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Oc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL71283 211061 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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.
ChEMBL 434 3 1 3 6.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Oc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL405289 219333 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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.
ChEMBL 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 10.1021/jm00099a019
10100280 103593 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL265073 103593 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
10346739 123805 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL338984 123805 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
10368075 175230 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL435019 175230 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
10436379 80954 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
CHEMBL20230 80954 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
10413997 9005 5 None - 2 Rat 4.8 pIC50 = 4.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
2246 9005 5 None - 2 Rat 4.8 pIC50 = 4.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL338522 9005 5 None - 2 Rat 4.8 pIC50 = 4.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
44336768 170131 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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
ChEMBL 599 7 3 4 6.1 O=C(O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL419183 170131 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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
ChEMBL 599 7 3 4 6.1 O=C(O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
11740743 20880 0 None - 3 Rat 7.8 pIC50 = 7.8 Binding
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
ChEMBL 384 3 1 2 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL119793 20880 0 None - 3 Rat 7.8 pIC50 = 7.8 Binding
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
ChEMBL 384 3 1 2 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm960133o
10495509 121905 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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
ChEMBL 314 1 1 2 4.2 Cc1cc(N)ccc1C(=O)N1CCCCc2cc(Cl)ccc21 10.1021/acs.jmedchem.5b00982
CHEMBL334376 121905 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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
ChEMBL 314 1 1 2 4.2 Cc1cc(N)ccc1C(=O)N1CCCCc2cc(Cl)ccc21 10.1021/acs.jmedchem.5b00982
23598641 101052 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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
ChEMBL 528 5 2 3 6.9 O=C(Nc1ccc(C(=O)N2CCC3(C=C(CO)CC3)Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2007.09.059
CHEMBL250346 101052 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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
ChEMBL 528 5 2 3 6.9 O=C(Nc1ccc(C(=O)N2CCC3(C=C(CO)CC3)Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2007.09.059
9974701 33435 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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
ChEMBL 342 4 1 2 5.1 CCCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL136177 33435 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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
ChEMBL 342 4 1 2 5.1 CCCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
10711405 126077 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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
ChEMBL 328 2 0 2 4.4 CN(C)c1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL343935 126077 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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
ChEMBL 328 2 0 2 4.4 CN(C)c1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
10810133 120580 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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
ChEMBL 385 3 2 2 5.3 O=C(Nc1ccccc1)Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL332450 120580 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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
ChEMBL 385 3 2 2 5.3 O=C(Nc1ccccc1)Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm960133o
44377894 126669 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 427 3 2 2 5.5 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1 10.1016/s0960-894x(02)01059-4
CHEMBL349062 126669 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 427 3 2 2 5.5 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1 10.1016/s0960-894x(02)01059-4
44332209 11093 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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
ChEMBL 470 3 1 2 6.9 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1Cl 10.1016/j.bmcl.2004.02.103
CHEMBL100893 11093 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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
ChEMBL 470 3 1 2 6.9 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1Cl 10.1016/j.bmcl.2004.02.103
10587836 126203 7 None - 1 Human 6.8 pIC50 = 6.8 Binding
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
ChEMBL 266 1 1 2 3.3 Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm000108p
CHEMBL344848 126203 7 None - 1 Human 6.8 pIC50 = 6.8 Binding
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
ChEMBL 266 1 1 2 3.3 Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm000108p
10524202 20534 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 386 4 1 3 4.5 COc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)cc1 10.1021/jm960133o
CHEMBL119534 20534 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 386 4 1 3 4.5 COc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)cc1 10.1021/jm960133o
10258045 25641 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL128219 25641 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
44352393 123643 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL338177 123643 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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
ChEMBL 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 10.1021/jm00077a002
9931699 81826 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 415 2 1 5 5.0 Cn1ccc(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(Cl)c2)n1 10.1016/j.bmcl.2005.10.107
CHEMBL203513 81826 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 415 2 1 5 5.0 Cn1ccc(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(Cl)c2)n1 10.1016/j.bmcl.2005.10.107
21467152 59931 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 478 3 1 3 6.9 O=C(Nc1ccc(C(=O)N2CCCCc3sc(Cl)cc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(00)00084-6
CHEMBL159831 59931 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 478 3 1 3 6.9 O=C(Nc1ccc(C(=O)N2CCCCc3sc(Cl)cc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(00)00084-6
15307999 108183 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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)
ChEMBL 492 3 1 3 7.1 O=C(Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(99)00278-4
CHEMBL297293 108183 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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)
ChEMBL 492 3 1 3 7.1 O=C(Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(99)00278-4
11792631 122006 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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
ChEMBL 356 4 0 2 5.2 CCN(CC)c1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL334688 122006 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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
ChEMBL 356 4 0 2 5.2 CCN(CC)c1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
44335357 114267 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 517 3 1 3 6.4 Cc1cc(F)cc(C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(CC5)N4Cc4ccccc43)c(Cl)c2)c1 10.1016/s0960-894x(02)00649-2
CHEMBL318530 114267 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 517 3 1 3 6.4 Cc1cc(F)cc(C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(CC5)N4Cc4ccccc43)c(Cl)c2)c1 10.1016/s0960-894x(02)00649-2
10550481 19647 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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
ChEMBL 428 4 2 4 4.6 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3N)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL118878 19647 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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
ChEMBL 428 4 2 4 4.6 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3N)cc2)c2ccccc21 10.1021/jm960133o
44377837 64308 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 427 3 2 2 5.5 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1 10.1016/s0960-894x(02)01059-4
CHEMBL166265 64308 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 427 3 2 2 5.5 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1 10.1016/s0960-894x(02)01059-4
10668163 20563 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 390 3 1 2 5.2 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccc(Cl)cc1 10.1021/jm960133o
CHEMBL119551 20563 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 390 3 1 2 5.2 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccc(Cl)cc1 10.1021/jm960133o
10054982 123723 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL338576 123723 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 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 10.1021/jm00077a002
10054203 124823 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL340388 124823 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL2112654 216022 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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.
ChEMBL 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 10.1021/jm00099a019
69940428 156650 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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.
ChEMBL 568 8 2 7 5.2 O=C(O)c1cccc(Cn2c(-c3ccc(Cl)cc3)nn(Cc3nnc(Cc4c(Cl)cccc4Cl)[nH]3)c2=O)c1 nan
CHEMBL3949118 156650 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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.
ChEMBL 568 8 2 7 5.2 O=C(O)c1cccc(Cn2c(-c3ccc(Cl)cc3)nn(Cc3nnc(Cc4c(Cl)cccc4Cl)[nH]3)c2=O)c1 nan
56848625 151971 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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.
ChEMBL 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 nan
CHEMBL3912406 151971 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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.
ChEMBL 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 nan
56848623 158460 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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.
ChEMBL 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 nan
CHEMBL3964135 158460 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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.
ChEMBL 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 nan
10673295 111673 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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
ChEMBL 509 3 1 3 6.9 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccc(Cl)cc1Cl 10.1021/jm980179c
CHEMBL311230 111673 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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
ChEMBL 509 3 1 3 6.9 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccc(Cl)cc1Cl 10.1021/jm980179c
10766720 112227 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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
ChEMBL 469 4 1 4 5.4 COc1cc(NC(=O)c2cc(F)ccc2C)ccc1C(=O)N1Cc2cccn2Cc2ccccc21 10.1021/jm980179c
CHEMBL312036 112227 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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
ChEMBL 469 4 1 4 5.4 COc1cc(NC(=O)c2cc(F)ccc2C)ccc1C(=O)N1Cc2cccn2Cc2ccccc21 10.1021/jm980179c
44378702 126869 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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
ChEMBL 657 7 1 5 7.8 CN(C)C1CCN(Cc2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1 10.1016/s0960-894x(00)00095-0
CHEMBL350869 126869 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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
ChEMBL 657 7 1 5 7.8 CN(C)C1CCN(Cc2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1 10.1016/s0960-894x(00)00095-0
9939024 139353 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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
ChEMBL 622 9 1 6 7.1 CN1CCCN(CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL369832 139353 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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
ChEMBL 622 9 1 6 7.1 CN1CCCN(CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
10503858 212336 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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
ChEMBL 453 3 1 3 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(C)c1 10.1021/jm980179c
CHEMBL81133 212336 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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
ChEMBL 453 3 1 3 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(C)c1 10.1021/jm980179c
44378703 64182 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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
ChEMBL 697 7 1 5 8.7 O=C(Nc1ccc(C(=O)N2Cc3ccc(CN4CCC(N5CCCCC5)CC4)n3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00095-0
CHEMBL165200 64182 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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
ChEMBL 697 7 1 5 8.7 O=C(Nc1ccc(C(=O)N2Cc3ccc(CN4CCC(N5CCCCC5)CC4)n3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00095-0
172997 9112 57 None - 2 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00084-6
2238 9112 57 None - 2 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00084-6
CHEMBL49429 9112 57 None - 2 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00084-6
DB06666 9112 57 None - 2 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00084-6
172997 9112 57 None - 2 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1021/jm980179c
2238 9112 57 None - 2 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1021/jm980179c
CHEMBL49429 9112 57 None - 2 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1021/jm980179c
DB06666 9112 57 None - 2 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1021/jm980179c
172997 9112 57 None - 2 Rat 8.6 pIC50 = 8.6 Binding
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.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(03)00388-3
2238 9112 57 None - 2 Rat 8.6 pIC50 = 8.6 Binding
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.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(03)00388-3
CHEMBL49429 9112 57 None - 2 Rat 8.6 pIC50 = 8.6 Binding
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.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(03)00388-3
DB06666 9112 57 None - 2 Rat 8.6 pIC50 = 8.6 Binding
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.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(03)00388-3
9935001 59924 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 483 4 1 3 6.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
CHEMBL159823 59924 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 483 4 1 3 6.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
9874047 126687 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
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
ChEMBL 631 9 1 5 7.3 CN(C)CCN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1Cl)C2 10.1016/s0960-894x(00)00095-0
CHEMBL349237 126687 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
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
ChEMBL 631 9 1 5 7.3 CN(C)CCN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1Cl)C2 10.1016/s0960-894x(00)00095-0
10459252 59425 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 517 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
CHEMBL159359 59425 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 517 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
44352776 28367 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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
ChEMBL 560 7 1 7 6.2 O=C(Nc1ccc(C(=O)N2CCC(CCn3cnnn3)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
CHEMBL131727 28367 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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
ChEMBL 560 7 1 7 6.2 O=C(Nc1ccc(C(=O)N2CCC(CCn3cnnn3)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
44336404 117736 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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
ChEMBL 568 7 2 4 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN(C)C)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL326225 117736 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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
ChEMBL 568 7 2 4 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN(C)C)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
10838492 20236 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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
ChEMBL 481 4 1 3 6.3 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3cc(Cl)cc(Cl)c3)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL119318 20236 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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
ChEMBL 481 4 1 3 6.3 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3cc(Cl)cc(Cl)c3)cc2)c2ccccc21 10.1021/jm960133o
9826033 64236 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 471 4 2 2 6.7 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL165670 64236 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 471 4 2 2 6.7 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
11239468 137466 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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
ChEMBL 704 10 1 6 8.3 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1OCCCC(=O)N1CCC(N2CCCCC2)CC1)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL368353 137466 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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
ChEMBL 704 10 1 6 8.3 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1OCCCC(=O)N1CCC(N2CCCCC2)CC1)c1ccccc1-c1ccccc1 10.1021/jm030287l
11167861 138127 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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
ChEMBL 495 5 1 4 6.7 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm00137a004
CHEMBL368791 138127 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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
ChEMBL 495 5 1 4 6.7 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm00137a004
10578000 175281 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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
ChEMBL 524 7 1 5 6.1 CN(C)CCN1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm030287l
CHEMBL435331 175281 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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
ChEMBL 524 7 1 5 6.1 CN(C)CCN1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm030287l
11386922 67214 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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
ChEMBL 525 6 1 5 6.7 COc1cc(C(=O)N2CCCC(N(C)C)c3sccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL175212 67214 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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
ChEMBL 525 6 1 5 6.7 COc1cc(C(=O)N2CCCC(N(C)C)c3sccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm030287l
9939929 174370 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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
ChEMBL 664 10 1 6 7.4 CN(C)C1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL430083 174370 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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
ChEMBL 664 10 1 6 7.4 CN(C)C1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
10548464 22154 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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
ChEMBL 390 3 1 2 5.2 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1cccc(Cl)c1 10.1021/jm960133o
CHEMBL121455 22154 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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
ChEMBL 390 3 1 2 5.2 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1cccc(Cl)c1 10.1021/jm960133o
10666852 119841 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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
ChEMBL 370 3 1 2 4.8 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL331164 119841 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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
ChEMBL 370 3 1 2 4.8 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
11270497 67213 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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
ChEMBL 435 4 2 2 5.9 O=C(Nc1ccc(C(=O)N2CCCCc3[nH]ccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm00137a004
CHEMBL175211 67213 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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
ChEMBL 435 4 2 2 5.9 O=C(Nc1ccc(C(=O)N2CCCCc3[nH]ccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm00137a004
11418441 176075 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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
ChEMBL 410 3 1 3 5.6 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1)c1ccccc1Cl 10.1021/jm00137a004
CHEMBL441498 176075 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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
ChEMBL 410 3 1 3 5.6 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1)c1ccccc1Cl 10.1021/jm00137a004
11272841 67574 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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
ChEMBL 550 7 1 5 6.6 O=C(Nc1ccc(C(=O)N2CCCN(CCN3CCCC3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL176146 67574 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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
ChEMBL 550 7 1 5 6.6 O=C(Nc1ccc(C(=O)N2CCCN(CCN3CCCC3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL2332717 216313 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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
ChEMBL 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 10.1016/j.bmcl.2012.12.041
10156521 79250 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 378 2 0 2 5.7 Cc1ccccc1-c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/j.bmcl.2005.08.007
CHEMBL198931 79250 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 378 2 0 2 5.7 Cc1ccccc1-c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/j.bmcl.2005.08.007
10347928 125244 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL341289 125244 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 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 10.1021/jm00077a002
10052468 27894 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL131235 27894 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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
ChEMBL 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 10.1021/jm00077a002
18917500 194224 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 423 3 2 5 3.9 Nc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
CHEMBL49392 194224 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 423 3 2 5 3.9 Nc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
10667727 17805 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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
ChEMBL 384 3 1 2 5.1 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)c(C)c1 10.1021/jm960133o
CHEMBL117566 17805 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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
ChEMBL 384 3 1 2 5.1 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)c(C)c1 10.1021/jm960133o
9935694 64160 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 499 4 1 3 7.0 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3CCCc4cn(C)c5cccc3c45)cc2)cc1 10.1016/s0960-894x(02)01059-4
CHEMBL165183 64160 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 499 4 1 3 7.0 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3CCCc4cn(C)c5cccc3c45)cc2)cc1 10.1016/s0960-894x(02)01059-4
10784361 122204 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1)N1CCCCc2cc(Cl)ccc21 10.1021/jm000108p
CHEMBL335040 122204 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1)N1CCCCc2cc(Cl)ccc21 10.1021/jm000108p
10834036 20407 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 386 4 1 3 4.5 COc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL119442 20407 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 386 4 1 3 4.5 COc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
10458629 25735 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL128712 25735 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 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 10.1021/jm00077a002
10029477 27483 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL130905 27483 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 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 10.1021/jm00077a002
10051081 123681 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL338383 123681 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 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 10.1021/jm00077a002
10256281 25676 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL128422 25676 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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
ChEMBL 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 10.1021/jm00077a002
56848626 150496 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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.
ChEMBL 557 9 2 7 4.2 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(Cc2ccccc2F)c1=O)c1ccccc1Cl nan
CHEMBL3900528 150496 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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.
ChEMBL 557 9 2 7 4.2 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(Cc2ccccc2F)c1=O)c1ccccc1Cl nan
10766187 19627 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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
ChEMBL 455 6 1 3 6.1 CCCN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL118863 19627 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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
ChEMBL 455 6 1 3 6.1 CCCN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
11798757 211067 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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.
ChEMBL 475 3 1 3 6.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(03)00388-3
CHEMBL71305 211067 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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.
ChEMBL 475 3 1 3 6.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(03)00388-3
10737018 37404 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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
ChEMBL 356 5 1 2 5.5 CCCCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL139415 37404 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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
ChEMBL 356 5 1 2 5.5 CCCCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
44374839 126947 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 442 3 1 5 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3cn(C)nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
CHEMBL351587 126947 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 442 3 1 5 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3cn(C)nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
44352373 29092 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL132389 29092 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 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 10.1021/jm00077a002
8105663 20201 5 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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
ChEMBL 356 3 1 2 4.5 O=C(Nc1ccccc1C(=O)N1CCCc2ccccc21)c1ccccc1 10.1021/jm960133o
CHEMBL119291 20201 5 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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
ChEMBL 356 3 1 2 4.5 O=C(Nc1ccccc1C(=O)N1CCCc2ccccc21)c1ccccc1 10.1021/jm960133o
44336379 114194 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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
ChEMBL 582 8 2 4 5.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCCN(C)C)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL318083 114194 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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
ChEMBL 582 8 2 4 5.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCCN(C)C)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
86690920 152320 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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.
ChEMBL 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 nan
CHEMBL3915055 152320 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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.
ChEMBL 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 nan
69940395 155857 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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.
ChEMBL 514 6 1 7 5.1 O=c1n(Cc2ncc(-c3ccccc3Cl)s2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3943019 155857 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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.
ChEMBL 514 6 1 7 5.1 O=c1n(Cc2ncc(-c3ccccc3Cl)s2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
87388676 158645 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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.
ChEMBL 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 nan
CHEMBL3965602 158645 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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.
ChEMBL 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 nan
2173 9730 13 None - 2 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity against Vasopressin V2 receptor was determined in Brattleboro ratsBinding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/jm020133q
3038506 9730 13 None - 2 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity against Vasopressin V2 receptor was determined in Brattleboro ratsBinding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/jm020133q
CHEMBL332447 9730 13 None - 2 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity against Vasopressin V2 receptor was determined in Brattleboro ratsBinding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/jm020133q
DB05838 9730 13 None - 2 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity against Vasopressin V2 receptor was determined in Brattleboro ratsBinding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/jm020133q
19699114 60150 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 434 3 1 5 4.9 Cn1cc2c(n1)-c1sccc1N(C(=O)c1ccc(NC(=O)C3CCCCC3)cc1)CC2 10.1016/s0960-894x(00)00084-6
CHEMBL160029 60150 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 434 3 1 5 4.9 Cn1cc2c(n1)-c1sccc1N(C(=O)c1ccc(NC(=O)C3CCCCC3)cc1)CC2 10.1016/s0960-894x(00)00084-6
14981577 85652 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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
ChEMBL 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 10.1021/jm00031a004
CHEMBL2112900 85652 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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
ChEMBL 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 10.1021/jm00031a004
2241 8999 1 None -208 4 Rat 5.6 pIC50 = 5.6 Binding
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.
ChEMBL None None None None 10.1021/jm00099a019
9810632 8999 1 None -208 4 Rat 5.6 pIC50 = 5.6 Binding
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.
ChEMBL None None None None 10.1021/jm00099a019
CHEMBL127686 8999 1 None -208 4 Rat 5.6 pIC50 = 5.6 Binding
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.
ChEMBL None None None None 10.1021/jm00099a019
44273425 105679 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
CHEMBL279281 105679 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
44273369 106320 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
CHEMBL283524 106320 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
10007685 105376 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL276906 105376 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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
ChEMBL 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 10.1021/jm00077a002
44374839 126947 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 442 3 1 5 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3cn(C)nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
CHEMBL351587 126947 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 442 3 1 5 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3cn(C)nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
10716676 117195 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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
ChEMBL 413 4 2 3 4.9 CNC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL324488 117195 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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
ChEMBL 413 4 2 3 4.9 CNC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
44293784 194676 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 444 3 1 4 4.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(F)ccc1F 10.1016/s0960-894x(99)00279-6
CHEMBL49657 194676 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 444 3 1 4 4.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(F)ccc1F 10.1016/s0960-894x(99)00279-6
71450903 85653 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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
ChEMBL 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 10.1021/jm00031a004
CHEMBL2112901 85653 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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
ChEMBL 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 10.1021/jm00031a004
71449109 85654 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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
ChEMBL 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 10.1021/jm00031a004
CHEMBL2112902 85654 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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
ChEMBL 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 10.1021/jm00031a004
10257352 85557 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL2112666 85557 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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
ChEMBL 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 10.1021/jm00077a002
10326385 162465 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL405016 162465 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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
ChEMBL 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 10.1021/jm00077a002
2168 10748 38 None -15 9 Human 6.6 pIC50 = 6.6 Binding
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
ChEMBL None None None None 10.1016/j.bmcl.2012.12.041
2810 10748 38 None -15 9 Human 6.6 pIC50 = 6.6 Binding
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
ChEMBL None None None None 10.1016/j.bmcl.2012.12.041
644077 10748 38 None -15 9 Human 6.6 pIC50 = 6.6 Binding
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
ChEMBL None None None None 10.1016/j.bmcl.2012.12.041
CHEMBL373742 10748 38 None -15 9 Human 6.6 pIC50 = 6.6 Binding
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
ChEMBL None None None None 10.1016/j.bmcl.2012.12.041
DB00067 10748 38 None -15 9 Human 6.6 pIC50 = 6.6 Binding
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
ChEMBL None None None None 10.1016/j.bmcl.2012.12.041
10647295 117051 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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
ChEMBL 452 5 1 4 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)CC#N)c3ccccc32)cc1 10.1021/jm960133o
CHEMBL323802 117051 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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
ChEMBL 452 5 1 4 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)CC#N)c3ccccc32)cc1 10.1021/jm960133o
44212554 110452 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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.
ChEMBL 432 3 1 2 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3ccccc3-c3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL308741 110452 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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.
ChEMBL 432 3 1 2 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3ccccc3-c3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
10622282 19938 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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
ChEMBL 424 3 1 2 5.8 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1021/jm960133o
CHEMBL119087 19938 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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
ChEMBL 424 3 1 2 5.8 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1021/jm960133o
22405331 142117 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 400 2 0 2 5.6 O=C(c1ccc(-c2cc(F)cc(F)c2)cc1)N1Cc2cccn2Cc2ccccc21 10.1016/j.bmcl.2005.08.007
CHEMBL372766 142117 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 400 2 0 2 5.6 O=C(c1ccc(-c2cc(F)cc(F)c2)cc1)N1Cc2cccn2Cc2ccccc21 10.1016/j.bmcl.2005.08.007
44273473 79559 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
CHEMBL20002 79559 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
10392579 123473 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL337221 123473 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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
ChEMBL 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 10.1021/jm00077a002
44352455 175409 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL436189 175409 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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
ChEMBL 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 10.1021/jm00077a002
2812 11551 101 None - 34 Human 5.6 pIC50 = 5.6 Binding
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
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
CHEMBL104 11551 101 None - 34 Human 5.6 pIC50 = 5.6 Binding
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
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
44335386 114787 0 None 14 2 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 489 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1F 10.1016/s0960-894x(02)00649-2
CHEMBL319433 114787 0 None 14 2 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 489 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1F 10.1016/s0960-894x(02)00649-2
44352171 27588 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL130993 27588 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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
ChEMBL 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 10.1021/jm00077a002
10366192 123470 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL337212 123470 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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
ChEMBL 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 10.1021/jm00077a002
53378951 151558 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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.
ChEMBL 507 6 1 5 5.7 O=c1n(Cc2cccc(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1CC(O)C(F)(F)F nan
CHEMBL3909196 151558 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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.
ChEMBL 507 6 1 5 5.7 O=c1n(Cc2cccc(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1CC(O)C(F)(F)F nan
10837161 18692 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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
ChEMBL 447 4 1 3 5.6 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3Cl)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL118270 18692 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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
ChEMBL 447 4 1 3 5.6 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3Cl)cc2)c2ccccc21 10.1021/jm960133o
10716675 121693 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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
ChEMBL 413 4 1 3 5.0 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL334225 121693 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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
ChEMBL 413 4 1 3 5.0 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3)cc2)c2ccccc21 10.1021/jm960133o
14981578 85648 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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
ChEMBL 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 10.1021/jm00031a004
CHEMBL2112897 85648 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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
ChEMBL 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 10.1021/jm00031a004
10074681 123831 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL339132 123831 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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
ChEMBL 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 10.1021/jm00077a002
2812 11551 101 None - 34 Human 5.6 pIC50 = 5.6 Binding
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
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
CHEMBL104 11551 101 None - 34 Human 5.6 pIC50 = 5.6 Binding
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
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
44332207 114039 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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
ChEMBL 504 3 1 2 7.6 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.02.103
CHEMBL316958 114039 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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
ChEMBL 504 3 1 2 7.6 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.02.103
53378730 159722 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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.
ChEMBL 548 7 1 7 5.4 O=c1n(Cc2nnc(Cc3ccccc3C(F)(F)F)[nH]2)nc(-c2ccc(Cl)s2)n1Cc1ccccc1F nan
CHEMBL3975038 159722 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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.
ChEMBL 548 7 1 7 5.4 O=c1n(Cc2nnc(Cc3ccccc3C(F)(F)F)[nH]2)nc(-c2ccc(Cl)s2)n1Cc1ccccc1F nan
10692266 20902 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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
ChEMBL 398 3 1 2 5.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL119806 20902 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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
ChEMBL 398 3 1 2 5.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCCc3ccccc32)cc1 10.1021/jm960133o
44335356 11997 0 None 5 2 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 385 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCNc3ccccc32)cc1 10.1016/s0960-894x(02)00649-2
CHEMBL106229 11997 0 None 5 2 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 385 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCNc3ccccc32)cc1 10.1016/s0960-894x(02)00649-2
44352185 28177 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL131477 28177 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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
ChEMBL 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 10.1021/jm00077a002
44272997 78496 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
CHEMBL19658 78496 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
10715974 18694 0 None - 2 Rat 7.5 pIC50 = 7.5 Binding
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
ChEMBL 400 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3ccccc32)cc1 10.1021/jm960133o
CHEMBL118271 18694 0 None - 2 Rat 7.5 pIC50 = 7.5 Binding
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
ChEMBL 400 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3ccccc32)cc1 10.1021/jm960133o
10835094 18858 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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
ChEMBL 404 3 1 2 5.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1Cl 10.1021/jm960133o
CHEMBL118387 18858 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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
ChEMBL 404 3 1 2 5.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1Cl 10.1021/jm960133o
10598596 19713 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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
ChEMBL 427 5 2 3 5.3 CCNC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL118922 19713 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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
ChEMBL 427 5 2 3 5.3 CCNC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
10743970 119842 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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
ChEMBL 499 7 1 5 5.2 CCOC(=O)CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL331173 119842 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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
ChEMBL 499 7 1 5 5.2 CCOC(=O)CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
22099567 108116 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
In vitro inhibition of [3H]AVP binding to rat V2 receptorIn vitro inhibition of [3H]AVP binding to rat V2 receptor
ChEMBL 457 3 1 4 5.6 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00278-4
CHEMBL296814 108116 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
In vitro inhibition of [3H]AVP binding to rat V2 receptorIn vitro inhibition of [3H]AVP binding to rat V2 receptor
ChEMBL 457 3 1 4 5.6 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00278-4
23598560 11223 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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
ChEMBL 512 4 1 2 7.9 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.02.103
CHEMBL101678 11223 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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
ChEMBL 512 4 1 2 7.9 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.02.103
44309960 211060 1 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1cccc(Cl)c1Cl 10.1016/s0960-894x(03)00388-3
CHEMBL71282 211060 1 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1cccc(Cl)c1Cl 10.1016/s0960-894x(03)00388-3
15307971 211336 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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.
ChEMBL 418 3 1 2 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3-c3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL72945 211336 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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.
ChEMBL 418 3 1 2 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3-c3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
18917519 194126 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 525 7 0 5 5.1 Cc1ccc(F)cc1C(=O)N(CCCN(C)C)c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
CHEMBL49323 194126 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 525 7 0 5 5.1 Cc1ccc(F)cc1C(=O)N(CCCN(C)C)c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
14981575 85647 0 None - 1 Rat 6.5 pIC50 = 6.5 Binding
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
ChEMBL 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 10.1021/jm00031a004
CHEMBL2112896 85647 0 None - 1 Rat 6.5 pIC50 = 6.5 Binding
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
ChEMBL 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 10.1021/jm00031a004
10483940 124052 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL339497 124052 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
9868852 82068 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 459 2 1 5 5.2 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(Br)c2)n1 10.1016/j.bmcl.2005.10.107
CHEMBL203739 82068 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 459 2 1 5 5.2 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(Br)c2)n1 10.1016/j.bmcl.2005.10.107
56848622 154718 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
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.
ChEMBL 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 nan
CHEMBL3933782 154718 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
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.
ChEMBL 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 nan
44293763 108285 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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
ChEMBL 422 3 1 4 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
CHEMBL297990 108285 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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
ChEMBL 422 3 1 4 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
9826254 170088 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(03)00388-3
CHEMBL418890 170088 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(03)00388-3
11763684 138135 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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
ChEMBL 650 9 1 6 7.0 CN1CCCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL368818 138135 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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
ChEMBL 650 9 1 6 7.0 CN1CCCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
9939929 174370 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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
ChEMBL 664 10 1 6 7.4 CN(C)C1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL430083 174370 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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
ChEMBL 664 10 1 6 7.4 CN(C)C1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
9826254 170088 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(00)00084-6
CHEMBL418890 170088 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(00)00084-6
9826254 170088 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1021/jm980179c
CHEMBL418890 170088 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1021/jm980179c
44374781 59955 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 486 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2CCCCc3sc(Cl)cc32)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
CHEMBL159856 59955 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 486 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2CCCCc3sc(Cl)cc32)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
9826254 170088 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
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
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1021/jm980179c
CHEMBL418890 170088 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
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
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1021/jm980179c
9826254 170088 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(00)00084-6
CHEMBL418890 170088 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(00)00084-6
69940338 157408 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
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.
ChEMBL 497 6 1 7 4.2 O=c1n(Cc2cn(-c3ccccc3Cl)cn2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3955416 157408 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
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.
ChEMBL 497 6 1 7 4.2 O=c1n(Cc2cn(-c3ccccc3Cl)cn2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
2168 10748 38 None - 9 Pig 8.5 pIC50 = 8.5 Binding
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
ChEMBL None None None None 10.1016/S0960-894X(97)00050-4
2810 10748 38 None - 9 Pig 8.5 pIC50 = 8.5 Binding
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
ChEMBL None None None None 10.1016/S0960-894X(97)00050-4
644077 10748 38 None - 9 Pig 8.5 pIC50 = 8.5 Binding
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
ChEMBL None None None None 10.1016/S0960-894X(97)00050-4
CHEMBL373742 10748 38 None - 9 Pig 8.5 pIC50 = 8.5 Binding
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
ChEMBL None None None None 10.1016/S0960-894X(97)00050-4
DB00067 10748 38 None - 9 Pig 8.5 pIC50 = 8.5 Binding
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
ChEMBL None None None None 10.1016/S0960-894X(97)00050-4
44374802 126781 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 442 3 1 3 6.1 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCCCc3sccc32)c(Cl)c1 10.1016/s0960-894x(00)00084-6
CHEMBL350089 126781 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 442 3 1 3 6.1 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCCCc3sccc32)c(Cl)c1 10.1016/s0960-894x(00)00084-6
20825285 115974 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 595 4 1 3 8.2 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(C5)N4Cc4cc(Cl)ccc43)c(Cl)c2)cc1 10.1016/s0960-894x(02)00649-2
CHEMBL321561 115974 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 595 4 1 3 8.2 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(C5)N4Cc4cc(Cl)ccc43)c(Cl)c2)cc1 10.1016/s0960-894x(02)00649-2
10578460 67205 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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
ChEMBL 544 6 1 5 7.1 O=C(Nc1ccc(C(=O)N2CCCN(Cc3cccnc3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL175182 67205 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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
ChEMBL 544 6 1 5 7.1 O=C(Nc1ccc(C(=O)N2CCCN(Cc3cccnc3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
11190868 67335 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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
ChEMBL 482 5 1 4 6.7 COc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CCCCc2sccc21 10.1021/jm00137a004
CHEMBL175930 67335 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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
ChEMBL 482 5 1 4 6.7 COc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CCCCc2sccc21 10.1021/jm00137a004
11190868 67335 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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
ChEMBL 482 5 1 4 6.7 COc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CCCCc2sccc21 10.1021/jm00137a004
CHEMBL175930 67335 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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
ChEMBL 482 5 1 4 6.7 COc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CCCCc2sccc21 10.1021/jm00137a004
11239468 137466 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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
ChEMBL 704 10 1 6 8.3 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1OCCCC(=O)N1CCC(N2CCCCC2)CC1)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL368353 137466 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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
ChEMBL 704 10 1 6 8.3 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1OCCCC(=O)N1CCC(N2CCCCC2)CC1)c1ccccc1-c1ccccc1 10.1021/jm030287l
11167861 138127 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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
ChEMBL 495 5 1 4 6.7 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm00137a004
CHEMBL368791 138127 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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
ChEMBL 495 5 1 4 6.7 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm00137a004
56848686 151316 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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.
ChEMBL 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 nan
CHEMBL3907257 151316 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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.
ChEMBL 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 nan
10762739 121160 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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
ChEMBL 386 3 1 3 4.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCOCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL333135 121160 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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
ChEMBL 386 3 1 3 4.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCOCc3ccccc32)cc1 10.1021/jm960133o
44404614 172529 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 378 2 0 2 5.7 Cc1ccc(-c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)cc1 10.1016/j.bmcl.2005.08.007
CHEMBL424663 172529 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 378 2 0 2 5.7 Cc1ccc(-c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)cc1 10.1016/j.bmcl.2005.08.007
119369 9384 74 None -1 8 Rat 6.5 pIC50 = 6.5 Binding
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
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm00137a004
2197 9384 74 None -1 8 Rat 6.5 pIC50 = 6.5 Binding
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
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm00137a004
4004 9384 74 None -1 8 Rat 6.5 pIC50 = 6.5 Binding
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
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm00137a004
CHEMBL420762 9384 74 None -1 8 Rat 6.5 pIC50 = 6.5 Binding
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
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm00137a004
11476070 67245 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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
ChEMBL 436 4 1 3 6.2 O=C(Nc1ccc(C(=O)N2CCCCc3occc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm00137a004
CHEMBL175411 67245 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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
ChEMBL 436 4 1 3 6.2 O=C(Nc1ccc(C(=O)N2CCCCc3occc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm00137a004
44273426 83881 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
CHEMBL20757 83881 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
44352311 25724 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL128652 25724 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
44352372 27414 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL130848 27414 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
10460052 28892 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL132211 28892 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
71449094 85554 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL2112663 85554 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
10392298 123591 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL337888 123591 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
9982888 175229 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL435009 175229 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
44273259 80295 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
CHEMBL20171 80295 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
11793558 35161 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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
ChEMBL 370 6 1 2 5.9 CCCCCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL137500 35161 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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
ChEMBL 370 6 1 2 5.9 CCCCCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
14981576 85645 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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
ChEMBL 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 10.1021/jm00031a004
CHEMBL2112894 85645 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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
ChEMBL 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 10.1021/jm00031a004
21467167 67308 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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
ChEMBL 452 4 1 3 6.7 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm00137a004
CHEMBL175813 67308 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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
ChEMBL 452 4 1 3 6.7 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm00137a004
CHEMBL1790937 215685 0 None - 2 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm00099a019
67412781 161051 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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.
ChEMBL 499 6 1 8 4.0 O=c1n(Cc2nnc(-c3ccccc3Cl)o2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3986461 161051 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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.
ChEMBL 499 6 1 8 4.0 O=c1n(Cc2nnc(-c3ccccc3Cl)o2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
10692311 170817 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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
ChEMBL 399 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N)c3ccccc32)cc1 10.1021/jm960133o
CHEMBL420880 170817 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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
ChEMBL 399 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N)c3ccccc32)cc1 10.1021/jm960133o
10591515 125661 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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
ChEMBL 316 2 0 2 4.5 O=C(c1ccc(-n2cccc2)cc1)N1CCCCc2ccccc21 10.1021/jm000108p
CHEMBL342251 125661 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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
ChEMBL 316 2 0 2 4.5 O=C(c1ccc(-n2cccc2)cc1)N1CCCCc2ccccc21 10.1021/jm000108p
44352164 25666 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL128383 25666 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
18917554 196600 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 497 5 1 5 4.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3ccc(CN(C)C)n3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
CHEMBL51645 196600 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 497 5 1 5 4.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3ccc(CN(C)C)n3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
21837085 109033 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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.
ChEMBL 421 3 1 3 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3cccn3-c3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL303176 109033 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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.
ChEMBL 421 3 1 3 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3cccn3-c3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
2173 9730 13 None 8 2 Human 6.5 pIC50 = 6.5 Binding
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
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/jm020133q
3038506 9730 13 None 8 2 Human 6.5 pIC50 = 6.5 Binding
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
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/jm020133q
CHEMBL332447 9730 13 None 8 2 Human 6.5 pIC50 = 6.5 Binding
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
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/jm020133q
DB05838 9730 13 None 8 2 Human 6.5 pIC50 = 6.5 Binding
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
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/jm020133q
CHEMBL126765 215447 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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.
ChEMBL 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 10.1021/jm00099a019
10483940 124052 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL339497 124052 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
44433367 96622 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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
ChEMBL 489 3 1 3 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CC3C=CC(=O)N3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2007.08.053
CHEMBL237772 96622 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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
ChEMBL 489 3 1 3 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CC3C=CC(=O)N3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2007.08.053
11157078 100970 7 None - 0 Human 7.5 pIC50 = 7.5 Binding
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
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL249741 100970 7 None - 0 Human 7.5 pIC50 = 7.5 Binding
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
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
10758700 31634 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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
ChEMBL 328 3 1 2 4.8 CCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL134525 31634 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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
ChEMBL 328 3 1 2 4.8 CCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
19699060 62921 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 466 3 2 4 5.4 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1)c1ccc(F)cc1Cl 10.1016/s0960-894x(00)00084-6
CHEMBL162588 62921 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 466 3 2 4 5.4 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1)c1ccc(F)cc1Cl 10.1016/s0960-894x(00)00084-6
44352442 170242 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL419973 170242 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 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 10.1021/jm00077a002
9937535 69812 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
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
ChEMBL 554 7 2 4 5.1 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL1788221 69812 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
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
ChEMBL 554 7 2 4 5.1 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
21837086 176229 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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.
ChEMBL 425 3 1 3 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1F 10.1016/s0960-894x(03)00388-3
CHEMBL442743 176229 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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.
ChEMBL 425 3 1 3 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1F 10.1016/s0960-894x(03)00388-3
10519373 123452 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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
ChEMBL 314 2 1 2 4.4 CNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL337098 123452 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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
ChEMBL 314 2 1 2 4.4 CNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
14981574 85649 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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
ChEMBL 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 10.1021/jm00031a004
CHEMBL2112898 85649 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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
ChEMBL 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 10.1021/jm00031a004
10483105 97455 1 None - 4 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat kidney V2 receptorInhibition of rat kidney V2 receptor
ChEMBL 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 10.1016/j.bmcl.2012.10.116
CHEMBL2391300 97455 1 None - 4 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat kidney V2 receptorInhibition of rat kidney V2 receptor
ChEMBL 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 10.1016/j.bmcl.2012.10.116
56848687 157260 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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.
ChEMBL 581 11 2 9 2.5 COCCn1c(-c2ccc(Cl)s2)nn(CC(=O)NCC(NS(C)(=O)=O)c2ccccc2C(F)(F)F)c1=O nan
CHEMBL3954357 157260 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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.
ChEMBL 581 11 2 9 2.5 COCCn1c(-c2ccc(Cl)s2)nn(CC(=O)NCC(NS(C)(=O)=O)c2ccccc2C(F)(F)F)c1=O nan
19699076 126984 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 500 3 2 4 6.0 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)c(Cl)c1)c1cc(Cl)ccc1F 10.1016/s0960-894x(00)00084-6
CHEMBL351970 126984 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 500 3 2 4 6.0 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)c(Cl)c1)c1cc(Cl)ccc1F 10.1016/s0960-894x(00)00084-6
44352441 27462 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL130887 27462 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
ChEMBL 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 10.1021/jm00077a002
5280343 195054 124 None -147 31 Human 4.4 pIC50 = 4.4 Binding
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
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL1520590 195054 124 None -147 31 Human 4.4 pIC50 = 4.4 Binding
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
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 195054 124 None -147 31 Human 4.4 pIC50 = 4.4 Binding
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
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
19699133 126709 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 496 3 1 5 5.9 Cn1cc2c(n1)-c1sccc1N(C(=O)c1ccc(NC(=O)c3ccc(Cl)cc3Cl)cc1)CC2 10.1016/s0960-894x(00)00084-6
CHEMBL349506 126709 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 496 3 1 5 5.9 Cn1cc2c(n1)-c1sccc1N(C(=O)c1ccc(NC(=O)c3ccc(Cl)cc3Cl)cc1)CC2 10.1016/s0960-894x(00)00084-6
44357890 175172 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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
ChEMBL 462 5 1 3 6.0 Cc1ccccc1OCC(=O)Nc1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(C)c1 10.1021/jm000108p
CHEMBL434654 175172 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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
ChEMBL 462 5 1 3 6.0 Cc1ccccc1OCC(=O)Nc1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(C)c1 10.1021/jm000108p
44332272 114016 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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
ChEMBL 450 3 1 2 6.6 Cc1cccc(C(=O)Nc2ccc(C(=O)N3CCC4(C=CCCC4)Cc4ccccc43)cc2)c1 10.1016/j.bmcl.2004.02.103
CHEMBL316849 114016 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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
ChEMBL 450 3 1 2 6.6 Cc1cccc(C(=O)Nc2ccc(C(=O)N3CCC4(C=CCCC4)Cc4ccccc43)cc2)c1 10.1016/j.bmcl.2004.02.103
11351397 67781 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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
ChEMBL 449 4 1 3 5.9 Cn1ccc2c1CCCCN2C(=O)c1ccc(NC(=O)c2ccccc2-c2ccccc2)cc1 10.1021/jm00137a004
CHEMBL176264 67781 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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
ChEMBL 449 4 1 3 5.9 Cn1ccc2c1CCCCN2C(=O)c1ccc(NC(=O)c2ccccc2-c2ccccc2)cc1 10.1021/jm00137a004
CHEMBL339118 218396 0 None -19 2 Rat 5.4 pIC50 = 5.4 Binding
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.
ChEMBL 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 10.1021/jm00099a019
44352496 26333 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL129983 26333 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
ChEMBL 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 10.1021/jm00077a002
23598598 11739 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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
ChEMBL 608 7 2 4 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL104839 11739 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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
ChEMBL 608 7 2 4 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
23598600 12139 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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
ChEMBL 594 7 2 4 5.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL106938 12139 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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
ChEMBL 594 7 2 4 5.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
11070458 24559 1 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against Vasopressin V2 receptor was determined in Brattleboro ratsBinding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
ChEMBL 453 5 1 3 5.4 CC(C)NC(=O)C[C@@H]1CCCN(C(=O)c2ccc(N3CCCC3)cc2Cl)c2ccccc21 10.1021/jm020133q
CHEMBL125878 24559 1 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against Vasopressin V2 receptor was determined in Brattleboro ratsBinding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
ChEMBL 453 5 1 3 5.4 CC(C)NC(=O)C[C@@H]1CCCN(C(=O)c2ccc(N3CCCC3)cc2Cl)c2ccccc21 10.1021/jm020133q
9801970 147498 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 415 2 1 5 5.1 Cc1ccnn1-c1ccc(C(=O)N2Cc3cccnc3Nc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2005.10.107
CHEMBL381763 147498 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 415 2 1 5 5.1 Cc1ccnn1-c1ccc(C(=O)N2Cc3cccnc3Nc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2005.10.107
44332168 11257 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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
ChEMBL 436 3 1 2 6.3 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1 10.1016/j.bmcl.2004.02.103
CHEMBL101935 11257 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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
ChEMBL 436 3 1 2 6.3 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1 10.1016/j.bmcl.2004.02.103
9799174 147351 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 364 2 0 2 5.4 O=C(c1ccc(-c2ccccc2)cc1)N1Cc2cccn2Cc2ccccc21 10.1016/j.bmcl.2005.08.007
CHEMBL381248 147351 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 364 2 0 2 5.4 O=C(c1ccc(-c2ccccc2)cc1)N1Cc2cccn2Cc2ccccc21 10.1016/j.bmcl.2005.08.007
44273316 105647 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
CHEMBL279022 105647 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 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 10.1016/0960-894X(94)00469-V
71720517 93782 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
CHEMBL2324200 93782 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
5280343 195054 124 None -147 31 Human 4.4 pIC50 = 4.4 Binding
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
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL1520590 195054 124 None -147 31 Human 4.4 pIC50 = 4.4 Binding
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
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 195054 124 None -147 31 Human 4.4 pIC50 = 4.4 Binding
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
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
44293777 194888 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 460 3 1 4 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1c(F)cccc1Cl 10.1016/s0960-894x(99)00279-6
CHEMBL49824 194888 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 460 3 1 4 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1c(F)cccc1Cl 10.1016/s0960-894x(99)00279-6
10837633 109801 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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
ChEMBL 459 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(F)cc1Cl 10.1021/jm980179c
CHEMBL306970 109801 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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
ChEMBL 459 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(F)cc1Cl 10.1021/jm980179c
10719289 212411 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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
ChEMBL 473 3 1 3 6.1 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1Cl 10.1021/jm980179c
CHEMBL81755 212411 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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
ChEMBL 473 3 1 3 6.1 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1Cl 10.1021/jm980179c
44214518 126677 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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
ChEMBL 561 5 2 4 7.0 O=C(Nc1ccc(C(=O)N2Cc3ccc(C(=O)O)n3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00095-0
CHEMBL349141 126677 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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
ChEMBL 561 5 2 4 7.0 O=C(Nc1ccc(C(=O)N2Cc3ccc(C(=O)O)n3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00095-0
10551037 211013 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 439 3 1 3 5.4 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
CHEMBL70981 211013 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 439 3 1 3 5.4 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
9954905 108689 4 None - 0 Rat 8.4 pIC50 = 8.4 Binding
In vitro inhibition of (P[3H]-AVP binding to isolated rat kidney medullary V2 receptorIn vitro inhibition of (P[3H]-AVP binding to isolated rat kidney medullary V2 receptor
ChEMBL 440 3 1 4 4.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
CHEMBL300946 108689 4 None - 0 Rat 8.4 pIC50 = 8.4 Binding
In vitro inhibition of (P[3H]-AVP binding to isolated rat kidney medullary V2 receptorIn vitro inhibition of (P[3H]-AVP binding to isolated rat kidney medullary V2 receptor
ChEMBL 440 3 1 4 4.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
10837633 109801 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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.
ChEMBL 459 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(F)cc1Cl 10.1016/s0960-894x(03)00388-3
CHEMBL306970 109801 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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.
ChEMBL 459 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(F)cc1Cl 10.1016/s0960-894x(03)00388-3
10551037 211013 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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.
ChEMBL 439 3 1 3 5.4 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL70981 211013 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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.
ChEMBL 439 3 1 3 5.4 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
10764664 211158 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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.
ChEMBL 421 3 1 3 5.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL71797 211158 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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.
ChEMBL 421 3 1 3 5.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
10231366 11726 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 561 4 1 3 7.7 O=C(Nc1ccc(C(=O)N2CC3C4CCC(CC4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
CHEMBL104796 11726 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 561 4 1 3 7.7 O=C(Nc1ccc(C(=O)N2CC3C4CCC(CC4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
9915472 176302 0 None 14 2 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 547 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
CHEMBL443498 176302 0 None 14 2 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 547 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
11422294 69080 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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
ChEMBL 636 8 1 6 6.6 CN(C)C1CCN(C(=O)COc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL177885 69080 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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
ChEMBL 636 8 1 6 6.6 CN(C)C1CCN(C(=O)COc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
10764664 211158 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 421 3 1 3 5.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
CHEMBL71797 211158 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 421 3 1 3 5.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
10495509 121905 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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
ChEMBL 314 1 1 2 4.2 Cc1cc(N)ccc1C(=O)N1CCCCc2cc(Cl)ccc21 10.1021/jm000108p
CHEMBL334376 121905 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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
ChEMBL 314 1 1 2 4.2 Cc1cc(N)ccc1C(=O)N1CCCCc2cc(Cl)ccc21 10.1021/jm000108p
10814200 170283 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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
ChEMBL 469 3 1 3 6.2 Cc1ccc(C)c(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)c1 10.1021/jm980179c
CHEMBL420216 170283 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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
ChEMBL 469 3 1 3 6.2 Cc1ccc(C)c(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)c1 10.1021/jm980179c
44293778 108397 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 476 3 1 4 5.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(Cl)ccc1Cl 10.1016/s0960-894x(99)00279-6
CHEMBL298911 108397 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 476 3 1 4 5.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(Cl)ccc1Cl 10.1016/s0960-894x(99)00279-6
69939726 151807 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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.
ChEMBL 498 6 1 8 3.6 O=c1n(Cc2cn(-c3ccccc3Cl)nn2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3911148 151807 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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.
ChEMBL 498 6 1 8 3.6 O=c1n(Cc2cn(-c3ccccc3Cl)nn2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
10742418 111263 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 455 3 1 3 5.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/jm980179c
CHEMBL310416 111263 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 455 3 1 3 5.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/jm980179c
53379068 149149 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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.
ChEMBL 551 7 2 6 5.4 O=C(O)c1ccc(-c2ccccc2Cl)cc1Cn1nc(-c2ccc(Cl)cc2)n(CC(O)C(F)(F)F)c1=O nan
CHEMBL3889504 149149 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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.
ChEMBL 551 7 2 6 5.4 O=C(O)c1ccc(-c2ccccc2Cl)cc1Cn1nc(-c2ccc(Cl)cc2)n(CC(O)C(F)(F)F)c1=O nan
10527151 108950 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 441 3 1 3 5.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1Cl 10.1021/jm980179c
CHEMBL302709 108950 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 441 3 1 3 5.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1Cl 10.1021/jm980179c
86690918 158599 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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.
ChEMBL 547 6 1 6 6.4 O=c1n(Cc2ccc(-c3cccc(Cl)c3Cl)s2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3965329 158599 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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.
ChEMBL 547 6 1 6 6.4 O=c1n(Cc2ccc(-c3cccc(Cl)c3Cl)s2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
69940091 154695 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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.
ChEMBL 508 6 1 6 5.1 O=c1n(Cc2ccnc(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3933604 154695 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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.
ChEMBL 508 6 1 6 5.1 O=c1n(Cc2ccnc(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
10548204 19156 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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
ChEMBL 386 4 1 3 4.5 COc1cccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)c1 10.1021/jm960133o
CHEMBL118562 19156 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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
ChEMBL 386 4 1 3 4.5 COc1cccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)c1 10.1021/jm960133o
10762667 19588 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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
ChEMBL 385 3 1 3 4.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCN(C)c3ccccc32)cc1 10.1021/jm960133o
CHEMBL118829 19588 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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
ChEMBL 385 3 1 3 4.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCN(C)c3ccccc32)cc1 10.1021/jm960133o
71720517 93782 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
CHEMBL2324200 93782 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
1307424 19207 12 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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
ChEMBL 356 3 1 2 4.5 O=C(Nc1cccc(C(=O)N2CCCc3ccccc32)c1)c1ccccc1 10.1021/jm960133o
CHEMBL118595 19207 12 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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
ChEMBL 356 3 1 2 4.5 O=C(Nc1cccc(C(=O)N2CCCc3ccccc32)c1)c1ccccc1 10.1021/jm960133o
CHEMBL419793 220020 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Concentration required to displace 50% of [3H]arginine vasopressin from rat kidney medullary (AVP-V2a site)Concentration required to displace 50% of [3H]arginine vasopressin from rat kidney medullary (AVP-V2a site)
ChEMBL 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](CCCCN)NC(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
10595449 17288 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
ChEMBL 372 3 1 3 4.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCOc3ccccc32)cc1 10.1021/jm960133o
CHEMBL116820 17288 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
ChEMBL 372 3 1 3 4.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCOc3ccccc32)cc1 10.1021/jm960133o
44272960 80040 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 527 6 1 5 3.2 CCNC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
CHEMBL20126 80040 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 527 6 1 5 3.2 CCNC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
11757133 123718 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
ChEMBL 543 6 2 5 2.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CC(=O)O)C1=O)C2 10.1021/jm00077a002
CHEMBL338548 123718 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
ChEMBL 543 6 2 5 2.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CC(=O)O)C1=O)C2 10.1021/jm00077a002
9889904 147124 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 449 2 1 5 5.5 Cc1ccnn1-c1ccc(C(=O)N2Cc3cccnc3Nc3ccccc32)c(C(F)(F)F)c1 10.1016/j.bmcl.2005.10.107
CHEMBL380733 147124 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 449 2 1 5 5.5 Cc1ccnn1-c1ccc(C(=O)N2Cc3cccnc3Nc3ccccc32)c(C(F)(F)F)c1 10.1016/j.bmcl.2005.10.107
44309820 211007 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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.
ChEMBL 433 3 2 3 6.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Nc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL70949 211007 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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.
ChEMBL 433 3 2 3 6.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Nc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
2981363 19295 7 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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
ChEMBL 390 3 1 2 5.2 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccccc1Cl 10.1021/jm960133o
CHEMBL118660 19295 7 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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
ChEMBL 390 3 1 2 5.2 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccccc1Cl 10.1021/jm960133o
10030231 25688 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
ChEMBL 541 6 1 4 4.5 CC(C)CC1NC(=O)N([C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1021/jm00077a002
CHEMBL128489 25688 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
ChEMBL 541 6 1 4 4.5 CC(C)CC1NC(=O)N([C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1021/jm00077a002
44352302 25730 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 521 6 1 4 6.7 CN(C)CC1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL128687 25730 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 521 6 1 4 6.7 CN(C)CC1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL1790938 215686 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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.
ChEMBL 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)N(C)C(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
10693776 16933 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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
ChEMBL 427 4 1 3 5.3 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCC(N(C)C)c4ccccc43)cc2)cc1 10.1021/jm960133o
CHEMBL115853 16933 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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
ChEMBL 427 4 1 3 5.3 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCC(N(C)C)c4ccccc43)cc2)cc1 10.1021/jm960133o
9935969 126930 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 505 4 2 2 7.3 O=C(Nc1ccc(C(=O)N2CCCc3c(Cl)[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL351453 126930 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 505 4 2 2 7.3 O=C(Nc1ccc(C(=O)N2CCCc3c(Cl)[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
23598642 161583 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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
ChEMBL 541 6 2 3 7.1 CNCC1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
CHEMBL400267 161583 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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
ChEMBL 541 6 2 3 7.1 CNCC1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
10460610 179409 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
ChEMBL 567 6 1 7 2.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CN(Cc3nn[nH]n3)C1=O)C2 10.1021/jm00077a002
CHEMBL449399 179409 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
ChEMBL 567 6 1 7 2.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CN(Cc3nn[nH]n3)C1=O)C2 10.1021/jm00077a002
14969548 208910 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 477 11 1 4 4.9 NCCCCCCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1 10.1021/jm00066a010
CHEMBL60905 208910 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 477 11 1 4 4.9 NCCCCCCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1 10.1021/jm00066a010
9937535 69812 1 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Evaluated for binding affinity towards vasopressin V2 receptor in ratEvaluated for binding affinity towards vasopressin V2 receptor in rat
ChEMBL 554 7 2 4 5.1 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL1788221 69812 1 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Evaluated for binding affinity towards vasopressin V2 receptor in ratEvaluated for binding affinity towards vasopressin V2 receptor in rat
ChEMBL 554 7 2 4 5.1 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
86690936 155906 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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.
ChEMBL 596 7 1 10 3.2 O=c1n(S(=O)(=O)c2ncnn2Cc2ccccc2C(F)(F)F)nc(-c2ccc(Cl)cc2)n1CC(O)C(F)(F)F nan
CHEMBL3943296 155906 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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.
ChEMBL 596 7 1 10 3.2 O=c1n(S(=O)(=O)c2ncnn2Cc2ccccc2C(F)(F)F)nc(-c2ccc(Cl)cc2)n1CC(O)C(F)(F)F nan
10461149 124058 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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
ChEMBL 596 7 4 8 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CNc3n[nH]c(N)n3)C1=O)C2 10.1021/jm00077a002
CHEMBL339524 124058 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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
ChEMBL 596 7 4 8 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CNc3n[nH]c(N)n3)C1=O)C2 10.1021/jm00077a002
44352413 28236 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
ChEMBL 549 7 2 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)Cc1cccnc1)C2 10.1021/jm00077a002
CHEMBL131551 28236 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
ChEMBL 549 7 2 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)Cc1cccnc1)C2 10.1021/jm00077a002
71720517 93782 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
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
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
CHEMBL2324200 93782 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
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
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
132072820 187712 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human AVPR2 by PathHunter beta-arrestin assayAntagonist activity at human AVPR2 by PathHunter beta-arrestin assay
ChEMBL 610 8 0 7 5.4 COC(=O)[C@H]1[C@@H](OCc2cccc(OC)c2)CC[C@H]2CN3CC[C@@]4(C(=O)N(Cc5cccc(OC)c5)c5ccccc54)[C@@H]3C[C@@H]21 10.1016/j.bmc.2020.115546
CHEMBL4758081 187712 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human AVPR2 by PathHunter beta-arrestin assayAntagonist activity at human AVPR2 by PathHunter beta-arrestin assay
ChEMBL 610 8 0 7 5.4 COC(=O)[C@H]1[C@@H](OCc2cccc(OC)c2)CC[C@H]2CN3CC[C@@]4(C(=O)N(Cc5cccc(OC)c5)c5ccccc54)[C@@H]3C[C@@H]21 10.1016/j.bmc.2020.115546
10369423 175358 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL435815 175358 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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
ChEMBL 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 10.1021/jm00077a002
44352400 25677 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 549 7 2 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)Cc1ccccn1)C2 10.1021/jm00077a002
CHEMBL128423 25677 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 549 7 2 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)Cc1ccccn1)C2 10.1021/jm00077a002
9910527 82693 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 429 2 0 5 5.2 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4N(C)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmcl.2005.10.107
CHEMBL205013 82693 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 429 2 0 5 5.2 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4N(C)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmcl.2005.10.107
56848684 155191 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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.
ChEMBL 545 9 2 7 3.9 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(CCC(F)(F)F)c1=O)c1ccccc1Cl nan
CHEMBL3937650 155191 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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.
ChEMBL 545 9 2 7 3.9 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(CCC(F)(F)F)c1=O)c1ccccc1Cl nan
44294195 108092 1 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 519 4 1 5 6.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(-c2ccccn2)ccc1Cl 10.1016/s0960-894x(99)00279-6
CHEMBL296619 108092 1 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 519 4 1 5 6.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(-c2ccccn2)ccc1Cl 10.1016/s0960-894x(99)00279-6
44352347 123584 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 540 6 4 7 2.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)c1n[nH]c(N)n1)C2 10.1021/jm00077a002
CHEMBL337853 123584 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 540 6 4 7 2.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)c1n[nH]c(N)n1)C2 10.1021/jm00077a002
44352184 123753 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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
ChEMBL 687 11 2 8 2.5 Cn1cnc(CC(=O)NC(CCS(C)(=O)=O)C(=O)N[C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)c1 10.1021/jm00077a002
CHEMBL338711 123753 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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
ChEMBL 687 11 2 8 2.5 Cn1cnc(CC(=O)NC(CCS(C)(=O)=O)C(=O)N[C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)c1 10.1021/jm00077a002
44352374 25299 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 529 7 3 5 3.0 CC(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 10.1021/jm00077a002
CHEMBL127445 25299 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 529 7 3 5 3.0 CC(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 10.1021/jm00077a002
9824954 80635 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 449 2 1 5 5.5 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2005.10.107
CHEMBL201889 80635 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 449 2 1 5 5.5 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2005.10.107
56848488 156334 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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.
ChEMBL 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)c1cccc(C(F)(F)F)c1 nan
CHEMBL3946734 156334 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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.
ChEMBL 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)c1cccc(C(F)(F)F)c1 nan
56848554 158624 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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.
ChEMBL 595 10 3 8 2.3 CS(=O)(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1Cl nan
CHEMBL3965460 158624 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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.
ChEMBL 595 10 3 8 2.3 CS(=O)(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1Cl nan
10503021 109513 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 435 3 1 3 5.6 Cc1cccc(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)c1C 10.1021/jm980179c
CHEMBL304956 109513 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 435 3 1 3 5.6 Cc1cccc(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)c1C 10.1021/jm980179c
172997 9112 57 None 64 2 Human 8.3 pIC50 = 8.3 Binding
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.09.059
2238 9112 57 None 64 2 Human 8.3 pIC50 = 8.3 Binding
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.09.059
CHEMBL49429 9112 57 None 64 2 Human 8.3 pIC50 = 8.3 Binding
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.09.059
DB06666 9112 57 None 64 2 Human 8.3 pIC50 = 8.3 Binding
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
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.09.059
54582950 69811 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Evaluated for binding affinity towards vasopressin V2 receptor in ratEvaluated for binding affinity towards vasopressin V2 receptor in rat
ChEMBL 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 10.1016/j.bmcl.2004.04.016
CHEMBL1788220 69811 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Evaluated for binding affinity towards vasopressin V2 receptor in ratEvaluated for binding affinity towards vasopressin V2 receptor in rat
ChEMBL 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 10.1016/j.bmcl.2004.04.016
10527151 108950 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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.
ChEMBL 441 3 1 3 5.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(03)00388-3
CHEMBL302709 108950 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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.
ChEMBL 441 3 1 3 5.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(03)00388-3
10642447 126078 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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
ChEMBL 362 3 1 2 5.4 CCNc1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL343945 126078 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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
ChEMBL 362 3 1 2 5.4 CCNc1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(Cl)c1 10.1021/jm000108p
172997 9112 57 None 64 2 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)00649-2
2238 9112 57 None 64 2 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)00649-2
CHEMBL49429 9112 57 None 64 2 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)00649-2
DB06666 9112 57 None 64 2 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)00649-2
44335329 174617 0 None 1 2 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 561 4 1 3 7.6 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(C5)N4Cc4cc(Cl)ccc43)cc2)cc1 10.1016/s0960-894x(02)00649-2
CHEMBL430841 174617 0 None 1 2 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 561 4 1 3 7.6 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(C5)N4Cc4cc(Cl)ccc43)cc2)cc1 10.1016/s0960-894x(02)00649-2
21467167 67308 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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
ChEMBL 452 4 1 3 6.7 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm00137a004
CHEMBL175813 67308 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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
ChEMBL 452 4 1 3 6.7 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm00137a004
9851013 127001 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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
ChEMBL 570 7 1 5 6.7 COc1cc(C(=O)N2Cc3ccc(CN(C)C)n3Cc3ccccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00095-0
CHEMBL352150 127001 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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
ChEMBL 570 7 1 5 6.7 COc1cc(C(=O)N2Cc3ccc(CN(C)C)n3Cc3ccccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00095-0
67408780 158908 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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.
ChEMBL 550 7 2 6 4.8 NC(=O)c1ccc(-c2ccccc2Cl)cc1Cn1nc(-c2ccc(Cl)cc2)n(CC(O)C(F)(F)F)c1=O nan
CHEMBL3967902 158908 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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.
ChEMBL 550 7 2 6 4.8 NC(=O)c1ccc(-c2ccccc2Cl)cc1Cn1nc(-c2ccc(Cl)cc2)n(CC(O)C(F)(F)F)c1=O nan
10831068 33982 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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
ChEMBL 340 4 1 2 4.9 C=CCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL136644 33982 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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
ChEMBL 340 4 1 2 4.9 C=CCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
10765617 19225 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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
ChEMBL 441 6 2 3 5.7 CCCNC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL118609 19225 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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
ChEMBL 441 6 2 3 5.7 CCCNC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
44377836 64307 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 505 4 2 2 7.3 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL166261 64307 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 505 4 2 2 7.3 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
11365307 68880 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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
ChEMBL 586 8 1 5 7.7 CN(CCc1cccnc1)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm00137a004
CHEMBL177556 68880 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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
ChEMBL 586 8 1 5 7.7 CN(CCc1cccnc1)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm00137a004
10840974 68553 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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
ChEMBL 579 7 1 6 5.8 CN1CCN(CCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccsc32)CC1 10.1021/jm030287l
CHEMBL177285 68553 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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
ChEMBL 579 7 1 6 5.8 CN1CCN(CCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccsc32)CC1 10.1021/jm030287l
11365307 68880 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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
ChEMBL 586 8 1 5 7.7 CN(CCc1cccnc1)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm00137a004
CHEMBL177556 68880 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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
ChEMBL 586 8 1 5 7.7 CN(CCc1cccnc1)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm00137a004
119369 9384 74 None 1 8 Human 6.3 pIC50 = 6.3 Binding
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
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm00137a004
2197 9384 74 None 1 8 Human 6.3 pIC50 = 6.3 Binding
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
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm00137a004
4004 9384 74 None 1 8 Human 6.3 pIC50 = 6.3 Binding
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
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm00137a004
CHEMBL420762 9384 74 None 1 8 Human 6.3 pIC50 = 6.3 Binding
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
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm00137a004
15307972 211128 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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.
ChEMBL 446 3 1 2 6.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL71626 211128 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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.
ChEMBL 446 3 1 2 6.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
71720517 93782 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
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
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
CHEMBL2324200 93782 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
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
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
10737785 34156 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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
ChEMBL 368 2 0 2 5.2 CC1CCN(c2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)C1 10.1021/jm000108p
CHEMBL136790 34156 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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
ChEMBL 368 2 0 2 5.2 CC1CCN(c2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)C1 10.1021/jm000108p
15298022 78815 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 370 2 0 3 5.4 O=C(c1ccc(-c2cccs2)cc1)N1Cc2cccn2Cc2ccccc21 10.1016/j.bmcl.2005.08.007
CHEMBL197616 78815 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 370 2 0 3 5.4 O=C(c1ccc(-c2cccs2)cc1)N1Cc2cccn2Cc2ccccc21 10.1016/j.bmcl.2005.08.007
71458039 85650 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 530 8 3 5 2.2 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@@H](N)CCC(N)=O)C2 10.1021/jm00031a004
CHEMBL2112899 85650 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 530 8 3 5 2.2 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@@H](N)CCC(N)=O)C2 10.1021/jm00031a004
10256467 27279 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 530 8 3 5 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)CCC(N)=O)C2 10.1021/jm00077a002
CHEMBL130742 27279 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 530 8 3 5 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)CCC(N)=O)C2 10.1021/jm00077a002
44352438 121999 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 541 6 3 5 3.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)C1CCCNC1)C2 10.1021/jm00077a002
CHEMBL334610 121999 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 541 6 3 5 3.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)C1CCCNC1)C2 10.1021/jm00077a002
44352412 122277 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 549 7 2 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)Cc1ccncc1)C2 10.1021/jm00077a002
CHEMBL335182 122277 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 549 7 2 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)Cc1ccncc1)C2 10.1021/jm00077a002
11269308 129391 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 390 3 1 3 5.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCc3sccc32)cc1 10.1021/jm00137a004
CHEMBL360272 129391 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 390 3 1 3 5.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCc3sccc32)cc1 10.1021/jm00137a004
CHEMBL1790937 215685 0 None - 2 Rat 5.3 pIC50 = 5.3 Binding
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.
ChEMBL 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 10.1021/jm00099a019
9984805 123836 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 541 7 2 4 4.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CCC1CCCNC1)C2 10.1021/jm00077a002
CHEMBL339155 123836 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 541 7 2 4 4.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CCC1CCCNC1)C2 10.1021/jm00077a002
11432362 100912 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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
ChEMBL 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 10.1016/j.bmcl.2007.09.059
CHEMBL249340 100912 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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
ChEMBL 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 10.1016/j.bmcl.2007.09.059
10621059 121039 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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
ChEMBL 401 4 1 4 4.4 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccccc1[N+](=O)[O-] 10.1021/jm960133o
CHEMBL333055 121039 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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
ChEMBL 401 4 1 4 4.4 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccccc1[N+](=O)[O-] 10.1021/jm960133o
44310140 211246 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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.
ChEMBL 423 3 2 4 4.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1O 10.1016/s0960-894x(03)00388-3
CHEMBL72342 211246 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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.
ChEMBL 423 3 2 4 4.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1O 10.1016/s0960-894x(03)00388-3
44352427 123592 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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
ChEMBL 637 10 4 6 3.2 CC(C)[C@H](NC(=O)Cc1c[nH]cn1)C(=O)NC[C@@]1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL337889 123592 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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
ChEMBL 637 10 4 6 3.2 CC(C)[C@H](NC(=O)Cc1c[nH]cn1)C(=O)NC[C@@]1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
10258572 124877 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 638 11 4 6 2.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CC(CC(N)=O)NC(=O)Cc1c[nH]cn1)C2 10.1021/jm00077a002
CHEMBL340676 124877 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 638 11 4 6 2.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CC(CC(N)=O)NC(=O)Cc1c[nH]cn1)C2 10.1021/jm00077a002
14969539 174740 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 434 8 0 3 5.2 CCCCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1 10.1021/jm00066a010
CHEMBL431723 174740 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 434 8 0 3 5.2 CCCCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1 10.1021/jm00066a010
44273321 174281 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 542 7 2 6 2.2 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(NCCN)C1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL429971 174281 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 542 7 2 6 2.2 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(NCCN)C1=O)C2 10.1016/0960-894X(94)00469-V
44377521 126857 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 571 7 1 5 7.0 CCOC(=O)Cn1cc2c3c(cccc31)N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccc(C)cc3)cc1)CCC2 10.1016/s0960-894x(02)01059-4
CHEMBL350792 126857 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 571 7 1 5 7.0 CCOC(=O)Cn1cc2c3c(cccc31)N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccc(C)cc3)cc1)CCC2 10.1016/s0960-894x(02)01059-4
23598556 11138 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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
ChEMBL 454 3 1 2 6.4 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1F 10.1016/j.bmcl.2004.02.103
CHEMBL101157 11138 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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
ChEMBL 454 3 1 2 6.4 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1F 10.1016/j.bmcl.2004.02.103
10459923 123120 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 539 5 1 4 3.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C1CN3CCC1CC3)C2 10.1021/jm00077a002
CHEMBL335944 123120 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 539 5 1 4 3.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C1CN3CCC1CC3)C2 10.1021/jm00077a002
10480543 123303 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 485 4 1 4 3.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1CCC(N)C1=O)C2 10.1021/jm00077a002
CHEMBL336195 123303 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 485 4 1 4 3.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1CCC(N)C1=O)C2 10.1021/jm00077a002
44352490 124730 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 577 6 2 6 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C1CC(S(C)(=O)=O)CN1)C2 10.1021/jm00077a002
CHEMBL340362 124730 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 577 6 2 6 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C1CC(S(C)(=O)=O)CN1)C2 10.1021/jm00077a002
44352443 125249 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 539 7 3 5 2.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)Cc1c[nH]cn1)C2 10.1021/jm00077a002
CHEMBL341311 125249 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 539 7 3 5 2.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)Cc1c[nH]cn1)C2 10.1021/jm00077a002
10437668 85655 1 None - 2 Rat 6.2 pIC50 = 6.2 Binding
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
ChEMBL 554 9 2 7 1.5 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@@H](N)CCS(C)(=O)=O)C3(C)C)CC1 10.1021/jm00031a004
CHEMBL2112903 85655 1 None - 2 Rat 6.2 pIC50 = 6.2 Binding
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
ChEMBL 554 9 2 7 1.5 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@@H](N)CCS(C)(=O)=O)C3(C)C)CC1 10.1021/jm00031a004
10415322 175019 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
ChEMBL 556 7 2 5 2.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CCC(N)=O)C1=O)C2 10.1021/jm00077a002
CHEMBL433662 175019 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
ChEMBL 556 7 2 5 2.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CCC(N)=O)C1=O)C2 10.1021/jm00077a002
2249 9008 18 None -54 6 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat kidney V2 receptorInhibition of rat kidney V2 receptor
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1016/j.bmcl.2012.10.116
9872389 9008 18 None -54 6 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat kidney V2 receptorInhibition of rat kidney V2 receptor
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1016/j.bmcl.2012.10.116
CHEMBL1253853 9008 18 None -54 6 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat kidney V2 receptorInhibition of rat kidney V2 receptor
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1016/j.bmcl.2012.10.116
10789935 18588 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Compound was tested for its ability to displace [3H]AVP from its specific binding sites in rat Kidney (AVP-V2 receptor).Compound was tested for its ability to displace [3H]AVP from its specific binding sites in rat Kidney (AVP-V2 receptor).
ChEMBL 455 4 1 5 5.0 CC(=O)O/N=C1\CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL118204 18588 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Compound was tested for its ability to displace [3H]AVP from its specific binding sites in rat Kidney (AVP-V2 receptor).Compound was tested for its ability to displace [3H]AVP from its specific binding sites in rat Kidney (AVP-V2 receptor).
ChEMBL 455 4 1 5 5.0 CC(=O)O/N=C1\CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
22405322 78557 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 406 4 0 2 6.3 CCCc1ccc(-c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)cc1 10.1016/j.bmcl.2005.08.007
CHEMBL196737 78557 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 406 4 0 2 6.3 CCCc1ccc(-c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)cc1 10.1016/j.bmcl.2005.08.007
9805201 63031 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 480 3 2 4 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)c(Cl)c1 10.1016/s0960-894x(00)00084-6
CHEMBL162748 63031 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 480 3 2 4 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)c(Cl)c1 10.1016/s0960-894x(00)00084-6
10279928 114132 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 527 4 1 3 7.0 O=C(Nc1ccc(C(=O)N2CC3C4CCC(CC4)N3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
CHEMBL317673 114132 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 527 4 1 3 7.0 O=C(Nc1ccc(C(=O)N2CC3C4CCC(CC4)N3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
11158261 136428 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
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
ChEMBL 692 12 1 6 8.1 CCN(CC)C1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL367323 136428 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
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
ChEMBL 692 12 1 6 8.1 CCN(CC)C1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
11490613 168517 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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
ChEMBL 636 9 1 6 6.6 CN1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL413748 168517 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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
ChEMBL 636 9 1 6 6.6 CN1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
10390899 193502 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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)
ChEMBL 490 3 1 3 6.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)c(Cl)c1 10.1016/s0960-894x(99)00278-4
CHEMBL48867 193502 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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)
ChEMBL 490 3 1 3 6.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)c(Cl)c1 10.1016/s0960-894x(99)00278-4
10578460 67205 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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
ChEMBL 544 6 1 5 7.1 O=C(Nc1ccc(C(=O)N2CCCN(Cc3cccnc3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL175182 67205 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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
ChEMBL 544 6 1 5 7.1 O=C(Nc1ccc(C(=O)N2CCCN(Cc3cccnc3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
11351397 67781 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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
ChEMBL 449 4 1 3 5.9 Cn1ccc2c1CCCCN2C(=O)c1ccc(NC(=O)c2ccccc2-c2ccccc2)cc1 10.1021/jm00137a004
CHEMBL176264 67781 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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
ChEMBL 449 4 1 3 5.9 Cn1ccc2c1CCCCN2C(=O)c1ccc(NC(=O)c2ccccc2-c2ccccc2)cc1 10.1021/jm00137a004
10392781 125055 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 549 7 2 5 4.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CCNC(=O)c1cccnc1)C2 10.1021/jm00077a002
CHEMBL340964 125055 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 549 7 2 5 4.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CCNC(=O)c1cccnc1)C2 10.1021/jm00077a002
3793 209988 77 None - 1 Human 5.2 pIC50 = 5.2 Binding
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
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 209988 77 None - 1 Human 5.2 pIC50 = 5.2 Binding
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
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 209988 77 None - 1 Human 5.2 pIC50 = 5.2 Binding
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
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
10620049 120883 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 384 5 1 2 4.9 O=C(CCc1ccccc1)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL332757 120883 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 384 5 1 2 4.9 O=C(CCc1ccccc1)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
44352392 123634 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 567 6 2 5 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)C1CN3CCC1CC3)C2 10.1021/jm00077a002
CHEMBL338118 123634 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 567 6 2 5 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)C1CN3CCC1CC3)C2 10.1021/jm00077a002
44273013 106246 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 543 7 2 6 2.2 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(NCCO)C1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL283126 106246 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 543 7 2 6 2.2 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(NCCO)C1=O)C2 10.1016/0960-894X(94)00469-V
10394512 123792 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
ChEMBL 652 11 3 7 2.3 Cn1cnc(CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)c1 10.1021/jm00077a002
CHEMBL338921 123792 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
ChEMBL 652 11 3 7 2.3 Cn1cnc(CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)c1 10.1021/jm00077a002
44352114 28836 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 517 8 3 5 2.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(N)CCCO)C2 10.1021/jm00077a002
CHEMBL132165 28836 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 517 8 3 5 2.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(N)CCCO)C2 10.1021/jm00077a002
10393719 29095 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 595 8 2 5 4.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CCNC(=O)CC1CN3CCC1CC3)C2 10.1021/jm00077a002
CHEMBL132391 29095 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 595 8 2 5 4.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CCNC(=O)CC1CN3CCC1CC3)C2 10.1021/jm00077a002
5280343 195054 124 None -147 31 Human 5.2 pIC50 = 5.2 Binding
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
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL1520590 195054 124 None -147 31 Human 5.2 pIC50 = 5.2 Binding
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
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 195054 124 None -147 31 Human 5.2 pIC50 = 5.2 Binding
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
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
3793 209988 77 None - 1 Human 5.2 pIC50 = 5.2 Binding
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
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 209988 77 None - 1 Human 5.2 pIC50 = 5.2 Binding
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
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 209988 77 None - 1 Human 5.2 pIC50 = 5.2 Binding
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
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
10790546 117424 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
ChEMBL 470 5 2 4 4.9 CC(=O)Nc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)C)c3ccccc32)cc1 10.1021/jm960133o
CHEMBL325819 117424 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
ChEMBL 470 5 2 4 4.9 CC(=O)Nc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)C)c3ccccc32)cc1 10.1021/jm960133o
2984025 19663 6 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 346 3 1 3 4.1 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccco1 10.1021/jm960133o
CHEMBL118892 19663 6 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 346 3 1 3 4.1 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccco1 10.1021/jm960133o
11764606 124142 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
ChEMBL 630 9 0 7 3.3 Cn1cnc(CC(=O)N(CCS(C)(=O)=O)[C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)c1 10.1021/jm00077a002
CHEMBL339756 124142 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
ChEMBL 630 9 0 7 3.3 Cn1cnc(CC(=O)N(CCS(C)(=O)=O)[C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)c1 10.1021/jm00077a002
2981862 120110 7 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 401 4 1 4 4.4 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccc([N+](=O)[O-])cc1 10.1021/jm960133o
CHEMBL331647 120110 7 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 401 4 1 4 4.4 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccc([N+](=O)[O-])cc1 10.1021/jm960133o
10414380 122843 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 521 6 1 4 4.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cc1ccccn1)C2 10.1021/jm00077a002
CHEMBL335634 122843 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 521 6 1 4 4.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cc1ccccn1)C2 10.1021/jm00077a002
44352124 123830 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 512 7 2 5 3.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(N)CCC#N)C2 10.1021/jm00077a002
CHEMBL339124 123830 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 512 7 2 5 3.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(N)CCC#N)C2 10.1021/jm00077a002
15340668 210548 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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.
ChEMBL 407 3 1 3 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3-c3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL68033 210548 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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.
ChEMBL 407 3 1 3 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3-c3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
10483586 27469 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
ChEMBL 591 7 1 6 2.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CCS(C)(=O)=O)C1=O)C2 10.1021/jm00077a002
CHEMBL130891 27469 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
ChEMBL 591 7 1 6 2.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CCS(C)(=O)=O)C1=O)C2 10.1021/jm00077a002
11757440 123707 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 556 7 1 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(CCC(=O)O)C1=O)C2 10.1021/jm00077a002
CHEMBL338503 123707 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 556 7 1 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(CCC(=O)O)C1=O)C2 10.1021/jm00077a002
53378840 156494 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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.
ChEMBL 532 6 1 7 5.3 O=c1n(Cc2cnc(-c3cccc(Cl)c3Cl)o2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3947893 156494 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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.
ChEMBL 532 6 1 7 5.3 O=c1n(Cc2cnc(-c3cccc(Cl)c3Cl)o2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
10322392 11463 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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
ChEMBL 468 3 1 2 6.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.02.103
CHEMBL103406 11463 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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
ChEMBL 468 3 1 2 6.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.02.103
10393965 28828 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 610 7 3 8 2.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CC(=O)Nc3nn[nH]n3)C1=O)C2 10.1021/jm00077a002
CHEMBL132157 28828 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 610 7 3 8 2.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CC(=O)Nc3nn[nH]n3)C1=O)C2 10.1021/jm00077a002
44352123 124869 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 566 8 3 6 1.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(N)CCS(N)(=O)=O)C2 10.1021/jm00077a002
CHEMBL340639 124869 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 566 8 3 6 1.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(N)CCS(N)(=O)=O)C2 10.1021/jm00077a002
15307968 109832 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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.
ChEMBL 432 3 1 2 6.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL307271 109832 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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.
ChEMBL 432 3 1 2 6.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
10619160 18617 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
ChEMBL 370 3 1 2 4.8 Cc1cccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)c1 10.1021/jm960133o
CHEMBL118220 18617 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
ChEMBL 370 3 1 2 4.8 Cc1cccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)c1 10.1021/jm960133o
44352453 25739 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 535 6 2 5 3.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)c1cccnc1)C2 10.1021/jm00077a002
CHEMBL128726 25739 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 535 6 2 5 3.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)c1cccnc1)C2 10.1021/jm00077a002
19699097 126782 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 446 3 2 4 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
CHEMBL350090 126782 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 446 3 2 4 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
CHEMBL435021 220440 2 None - 2 Rat 6.2 pIC50 = 6.2 Binding
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.
ChEMBL 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]2CNCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
9871426 123789 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 522 6 2 4 6.6 O=C(O)CC1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL338901 123789 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 522 6 2 4 6.6 O=C(O)CC1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
44352757 125232 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 522 6 2 4 6.6 O=C(O)C[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL341173 125232 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 522 6 2 4 6.6 O=C(O)C[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
44378885 126885 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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
ChEMBL 625 7 1 6 6.4 COc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1Cc2ccc(CN3CCN(C)CC3)n2Cc2ccccc21 10.1016/s0960-894x(00)00095-0
CHEMBL351019 126885 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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
ChEMBL 625 7 1 6 6.4 COc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1Cc2ccc(CN3CCN(C)CC3)n2Cc2ccccc21 10.1016/s0960-894x(00)00095-0
18917534 211073 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
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.
ChEMBL 485 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1Br 10.1016/s0960-894x(03)00388-3
CHEMBL71355 211073 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
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.
ChEMBL 485 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1Br 10.1016/s0960-894x(03)00388-3
10392505 115369 0 None 4 2 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 539 3 1 3 6.6 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(02)00649-2
CHEMBL320416 115369 0 None 4 2 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 539 3 1 3 6.6 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(02)00649-2
11490514 137467 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
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
ChEMBL 622 10 1 6 7.1 CN1CCN(CCCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL368354 137467 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
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
ChEMBL 622 10 1 6 7.1 CN1CCN(CCCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
44294175 108616 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 520 3 1 4 5.8 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(Br)ccc1Cl 10.1016/s0960-894x(99)00279-6
CHEMBL300433 108616 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 520 3 1 4 5.8 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(Br)ccc1Cl 10.1016/s0960-894x(99)00279-6
9959838 172325 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 574 6 1 4 7.3 CN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1Cl)C2 10.1016/s0960-894x(00)00095-0
CHEMBL424163 172325 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 574 6 1 4 7.3 CN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1Cl)C2 10.1016/s0960-894x(00)00095-0
10831734 125660 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 350 2 0 2 5.1 O=C(c1ccc(-n2cccc2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
CHEMBL342250 125660 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 350 2 0 2 5.1 O=C(c1ccc(-n2cccc2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
67409800 153676 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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.
ChEMBL 497 6 1 7 4.2 O=c1n(Cc2cnn(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3925572 153676 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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.
ChEMBL 497 6 1 7 4.2 O=c1n(Cc2cnn(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
56848491 159198 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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.
ChEMBL 651 9 3 8 4.7 CC(C)(C)OC(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1C(F)(F)F nan
CHEMBL3970631 159198 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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.
ChEMBL 651 9 3 8 4.7 CC(C)(C)OC(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1C(F)(F)F nan
10595343 121202 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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
ChEMBL 370 3 1 2 4.9 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1 10.1021/jm960133o
CHEMBL333201 121202 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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
ChEMBL 370 3 1 2 4.9 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1 10.1021/jm960133o
44332273 175896 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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
ChEMBL 450 3 1 2 6.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.02.103
CHEMBL440147 175896 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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
ChEMBL 450 3 1 2 6.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.02.103
10626339 135427 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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
ChEMBL 543 6 1 4 7.7 O=C(Nc1ccc(C(=O)N2CCCN(Cc3ccccc3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL366790 135427 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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
ChEMBL 543 6 1 4 7.7 O=C(Nc1ccc(C(=O)N2CCCN(Cc3ccccc3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
5280343 195054 124 None -147 31 Human 5.2 pIC50 = 5.2 Binding
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
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL1520590 195054 124 None -147 31 Human 5.2 pIC50 = 5.2 Binding
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
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 195054 124 None -147 31 Human 5.2 pIC50 = 5.2 Binding
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
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
9981665 125255 4 None -77 6 Rat 4.2 pIC50 = 4.2 Binding
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
ChEMBL 459 5 2 4 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CC(=O)O)C2 10.1021/jm00077a002
CHEMBL341339 125255 4 None -77 6 Rat 4.2 pIC50 = 4.2 Binding
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
ChEMBL 459 5 2 4 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CC(=O)O)C2 10.1021/jm00077a002
11798122 121310 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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
ChEMBL 458 5 1 5 4.9 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3[N+](=O)[O-])cc2)c2ccccc21 10.1021/jm960133o
CHEMBL333597 121310 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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
ChEMBL 458 5 1 5 4.9 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3[N+](=O)[O-])cc2)c2ccccc21 10.1021/jm960133o
11238362 175687 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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
ChEMBL 562 6 2 4 6.5 CCOc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL438523 175687 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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
ChEMBL 562 6 2 4 6.5 CCOc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
19699097 126782 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 446 3 2 4 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
CHEMBL350090 126782 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 446 3 2 4 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
977621 16861 12 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 322 4 1 2 4.0 CCCC(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL115434 16861 12 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
ChEMBL 322 4 1 2 4.0 CCCC(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
44273173 105801 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 555 7 0 5 4.0 CCN(CC)[C@@H]1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
CHEMBL280202 105801 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 555 7 0 5 4.0 CCN(CC)[C@@H]1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
44335241 174777 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 575 4 1 3 8.0 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(CC5)N4Cc4cc(Cl)ccc43)cc2)cc1 10.1016/s0960-894x(02)00649-2
CHEMBL432009 174777 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 575 4 1 3 8.0 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(CC5)N4Cc4cc(Cl)ccc43)cc2)cc1 10.1016/s0960-894x(02)00649-2
CHEMBL2112250 216016 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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.
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
44273034 105824 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 557 7 2 6 2.3 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(NCC(=O)O)C1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL280356 105824 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 557 7 2 6 2.3 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(NCC(=O)O)C1=O)C2 10.1016/0960-894X(94)00469-V
14969534 174663 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 412 2 0 2 4.0 O=C(c1ccc(Br)cc1)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1021/jm00066a010
CHEMBL431159 174663 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 412 2 0 2 4.0 O=C(c1ccc(Br)cc1)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1021/jm00066a010
9986160 124148 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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
ChEMBL 608 7 2 6 3.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CN(CC(=O)Nc3ncc[nH]3)C1=O)C2 10.1021/jm00077a002
CHEMBL339768 124148 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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
ChEMBL 608 7 2 6 3.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CN(CC(=O)Nc3ncc[nH]3)C1=O)C2 10.1021/jm00077a002
CHEMBL2112655 216023 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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.
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
44352146 123995 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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
ChEMBL 513 5 2 5 2.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CN1C(=O)CNC1=O)C2 10.1021/jm00077a002
CHEMBL339433 123995 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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
ChEMBL 513 5 2 5 2.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CN1C(=O)CNC1=O)C2 10.1021/jm00077a002
44352491 125007 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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
ChEMBL 549 8 2 5 2.7 C[S+]([O-])CCC(N)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL340915 125007 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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
ChEMBL 549 8 2 5 2.7 C[S+]([O-])CCC(N)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL2112651 216021 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Concentration required to displace 50% of [3H]arginine vasopressin from rat kidney medullary (AVP-V2a site)Concentration required to displace 50% of [3H]arginine vasopressin from rat kidney medullary (AVP-V2a site)
ChEMBL 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]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
10369550 125254 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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
ChEMBL 524 6 1 5 3.6 Cn1cncc1CC(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL341338 125254 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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
ChEMBL 524 6 1 5 3.6 Cn1cncc1CC(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
44444760 161398 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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
ChEMBL 518 4 2 3 6.1 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3Cl)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
CHEMBL399288 161398 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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
ChEMBL 518 4 2 3 6.1 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3Cl)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
10501216 119910 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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
ChEMBL 401 4 1 4 4.4 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1cccc([N+](=O)[O-])c1 10.1021/jm960133o
CHEMBL331424 119910 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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
ChEMBL 401 4 1 4 4.4 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1cccc([N+](=O)[O-])c1 10.1021/jm960133o
10713341 19727 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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
ChEMBL 357 3 1 3 3.9 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1cccnc1 10.1021/jm960133o
CHEMBL118933 19727 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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
ChEMBL 357 3 1 3 3.9 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1cccnc1 10.1021/jm960133o
10599369 121590 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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
ChEMBL 443 5 1 4 5.0 COc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)C)c3ccccc32)cc1 10.1021/jm960133o
CHEMBL334082 121590 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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
ChEMBL 443 5 1 4 5.0 COc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)C)c3ccccc32)cc1 10.1021/jm960133o
21837089 110587 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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.
ChEMBL 451 5 1 4 5.3 CCOc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL309096 110587 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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.
ChEMBL 451 5 1 4 5.3 CCOc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
14969514 210091 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 368 2 0 2 3.9 O=C(c1ccc(Cl)cc1)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1021/jm00066a010
CHEMBL64811 210091 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 368 2 0 2 3.9 O=C(c1ccc(Cl)cc1)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1021/jm00066a010
10548205 19480 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Compound was tested for its ability to displace [3H]AVP from its specific binding sites in rat Kidney (AVP-V2 receptor).Compound was tested for its ability to displace [3H]AVP from its specific binding sites in rat Kidney (AVP-V2 receptor).
ChEMBL 386 3 1 3 5.3 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)Oc1ccccc1 10.1021/jm960133o
CHEMBL118760 19480 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Compound was tested for its ability to displace [3H]AVP from its specific binding sites in rat Kidney (AVP-V2 receptor).Compound was tested for its ability to displace [3H]AVP from its specific binding sites in rat Kidney (AVP-V2 receptor).
ChEMBL 386 3 1 3 5.3 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)Oc1ccccc1 10.1021/jm960133o
10075696 28313 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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
ChEMBL 530 8 3 5 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@@H](N)CCC(N)=O)C2 10.1021/jm00077a002
CHEMBL131650 28313 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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
ChEMBL 530 8 3 5 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@@H](N)CCC(N)=O)C2 10.1021/jm00077a002
3793 209988 77 None - 1 Human 6.1 pIC50 = 6.1 Binding
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
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 209988 77 None - 1 Human 6.1 pIC50 = 6.1 Binding
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
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 209988 77 None - 1 Human 6.1 pIC50 = 6.1 Binding
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
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
9828129 123399 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 522 6 2 4 6.6 O=C(O)C[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL336825 123399 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 522 6 2 4 6.6 O=C(O)C[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
44352783 123559 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 508 6 2 4 6.5 O=C(Nc1ccc(C(=O)N2CCC(CCO)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
CHEMBL337725 123559 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 508 6 2 4 6.5 O=C(Nc1ccc(C(=O)N2CCC(CCO)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
23598598 11739 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human V2 receptor (Compound 7o)Binding affinity measured by inhibition of 3[H] AVP binding to cloned human V2 receptor (Compound 7o)
ChEMBL 608 7 2 4 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL104839 11739 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human V2 receptor (Compound 7o)Binding affinity measured by inhibition of 3[H] AVP binding to cloned human V2 receptor (Compound 7o)
ChEMBL 608 7 2 4 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
54582950 69811 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 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 10.1016/j.bmcl.2004.04.016
CHEMBL1788220 69811 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 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 10.1016/j.bmcl.2004.04.016
56848555 158528 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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.
ChEMBL 560 9 4 7 2.5 NC(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1Cl nan
CHEMBL3964694 158528 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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.
ChEMBL 560 9 4 7 2.5 NC(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1Cl nan
9848300 126836 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 487 4 2 3 6.1 O=C(Nc1ccc(C(=O)N2CCCC3C(=O)Nc4cccc2c43)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL350576 126836 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 487 4 2 3 6.1 O=C(Nc1ccc(C(=O)N2CCCC3C(=O)Nc4cccc2c43)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
10743659 212481 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 489 3 1 3 6.6 Cc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1NC(=O)c1ccc(Cl)cc1Cl 10.1021/jm980179c
CHEMBL82376 212481 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 489 3 1 3 6.6 Cc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1NC(=O)c1ccc(Cl)cc1Cl 10.1021/jm980179c
44444762 161508 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 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 10.1016/j.bmcl.2007.09.059
CHEMBL399888 161508 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 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 10.1016/j.bmcl.2007.09.059
11262100 68548 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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
ChEMBL 624 13 1 6 7.3 CN(C)CCN(C)CCCCOc1cc(C(=O)N2CCCCc3sccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL177248 68548 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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
ChEMBL 624 13 1 6 7.3 CN(C)CCN(C)CCCCOc1cc(C(=O)N2CCCCc3sccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm030287l
11422294 69080 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 636 8 1 6 6.6 CN(C)C1CCN(C(=O)COc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL177885 69080 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 636 8 1 6 6.6 CN(C)C1CCN(C(=O)COc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
86690917 157190 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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.
ChEMBL 555 8 2 9 2.7 NC(=O)Cn1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nc1-c1ccccc1Cl nan
CHEMBL3953766 157190 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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.
ChEMBL 555 8 2 9 2.7 NC(=O)Cn1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nc1-c1ccccc1Cl nan
18917553 108239 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 484 4 1 4 6.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(99)00279-6
CHEMBL297705 108239 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 484 4 1 4 6.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(99)00279-6
10673699 113461 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 527 3 1 3 6.8 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1cccc(C(F)(F)F)c1F 10.1021/jm980179c
CHEMBL314344 113461 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 527 3 1 3 6.8 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1cccc(C(F)(F)F)c1F 10.1021/jm980179c
10673295 111673 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 509 3 1 3 6.9 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccc(Cl)cc1Cl 10.1021/jm980179c
CHEMBL311230 111673 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 509 3 1 3 6.9 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccc(Cl)cc1Cl 10.1021/jm980179c
86690931 155808 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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.
ChEMBL 543 6 1 7 5.1 O=c1n(Cc2cc(-c3cccc(Cl)c3Cl)ncn2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3942564 155808 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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.
ChEMBL 543 6 1 7 5.1 O=c1n(Cc2cc(-c3cccc(Cl)c3Cl)ncn2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
71146879 152913 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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.
ChEMBL 498 6 2 7 3.8 O=c1n(Cc2nnc(-c3ccccc3Cl)[nH]2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3919631 152913 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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.
ChEMBL 498 6 2 7 3.8 O=c1n(Cc2nnc(-c3ccccc3Cl)[nH]2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
44378675 175417 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 671 6 1 5 7.4 CN(C)C1CCN(C(=O)c2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1 10.1016/s0960-894x(00)00095-0
CHEMBL436241 175417 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 671 6 1 5 7.4 CN(C)C1CCN(C(=O)c2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1 10.1016/s0960-894x(00)00095-0
10569977 37751 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 351 2 0 3 4.5 O=C(c1ccc(-n2cccn2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
CHEMBL139863 37751 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 351 2 0 3 4.5 O=C(c1ccc(-n2cccn2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
3537 10776 22 None 3 3 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1016/j.bmcl.2005.10.107
5311500 10776 22 None 3 3 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1016/j.bmcl.2005.10.107
CHEMBL363910 10776 22 None 3 3 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1016/j.bmcl.2005.10.107
11262100 68548 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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
ChEMBL 624 13 1 6 7.3 CN(C)CCN(C)CCCCOc1cc(C(=O)N2CCCCc3sccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL177248 68548 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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
ChEMBL 624 13 1 6 7.3 CN(C)CCN(C)CCCCOc1cc(C(=O)N2CCCCc3sccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm030287l
10626339 135427 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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
ChEMBL 543 6 1 4 7.7 O=C(Nc1ccc(C(=O)N2CCCN(Cc3ccccc3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL366790 135427 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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
ChEMBL 543 6 1 4 7.7 O=C(Nc1ccc(C(=O)N2CCCN(Cc3ccccc3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
10578000 175281 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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
ChEMBL 524 7 1 5 6.1 CN(C)CCN1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm030287l
CHEMBL435331 175281 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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
ChEMBL 524 7 1 5 6.1 CN(C)CCN1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm030287l
3537 10776 22 None 3 3 Human 7.1 pIC50 = 7.1 Binding
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
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1016/j.bmcl.2007.08.053
5311500 10776 22 None 3 3 Human 7.1 pIC50 = 7.1 Binding
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
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1016/j.bmcl.2007.08.053
CHEMBL363910 10776 22 None 3 3 Human 7.1 pIC50 = 7.1 Binding
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
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1016/j.bmcl.2007.08.053
3793 209988 77 None - 1 Human 6.1 pIC50 = 6.1 Binding
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
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 209988 77 None - 1 Human 6.1 pIC50 = 6.1 Binding
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
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 209988 77 None - 1 Human 6.1 pIC50 = 6.1 Binding
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
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
14969540 107585 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 362 3 0 2 3.8 CCc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1 10.1021/jm00066a010
CHEMBL293184 107585 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 362 3 0 2 3.8 CCc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1 10.1021/jm00066a010
CHEMBL2112249 216015 1 None - 2 Rat 6.1 pIC50 = 6.1 Binding
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
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
11764710 123217 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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
ChEMBL 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](CCC(N)=O)NC(=O)Cc1c[nH]cn1)C2 10.1021/jm00077a002
CHEMBL336082 123217 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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
ChEMBL 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](CCC(N)=O)NC(=O)Cc1c[nH]cn1)C2 10.1021/jm00077a002
5099582 117283 9 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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
ChEMBL 322 3 1 2 3.9 CC(C)C(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL324935 117283 9 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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
ChEMBL 322 3 1 2 3.9 CC(C)C(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL52813 222484 0 None -23 2 Rat 4.1 pIC50 = 4.1 Binding
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.
ChEMBL 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]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/jm00099a019
10741034 20708 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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
ChEMBL 424 3 1 2 5.8 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1cc(Cl)cc(Cl)c1 10.1021/jm960133o
CHEMBL119651 20708 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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
ChEMBL 424 3 1 2 5.8 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1cc(Cl)cc(Cl)c1 10.1021/jm960133o
14969542 207331 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 390 5 0 2 4.6 CCCCc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1 10.1021/jm00066a010
CHEMBL59900 207331 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 390 5 0 2 4.6 CCCCc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1 10.1021/jm00066a010
44273417 106283 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 555 7 0 5 4.0 CCN(CC)[C@H]1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
CHEMBL283317 106283 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 555 7 0 5 4.0 CCN(CC)[C@H]1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
10370127 25643 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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
ChEMBL 542 6 2 5 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CN1CC[C@H](N)C1=O)C2 10.1021/jm00077a002
CHEMBL128228 25643 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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
ChEMBL 542 6 2 5 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CN1CC[C@H](N)C1=O)C2 10.1021/jm00077a002
44352796 28248 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 510 6 1 3 7.5 O=C(Nc1ccc(C(=O)N2CCC(CCF)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
CHEMBL131566 28248 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 510 6 1 3 7.5 O=C(Nc1ccc(C(=O)N2CCC(CCF)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
15307967 109068 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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.
ChEMBL 432 3 1 2 6.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL303376 109068 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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.
ChEMBL 432 3 1 2 6.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
15307988 211141 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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.
ChEMBL 450 3 1 3 6.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Sc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL71712 211141 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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.
ChEMBL 450 3 1 3 6.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Sc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
10393977 175300 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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
ChEMBL 611 10 3 5 3.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)N(CCC(=O)O)CCc1c[nH]cn1)C2 10.1021/jm00077a002
CHEMBL435409 175300 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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
ChEMBL 611 10 3 5 3.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)N(CCC(=O)O)CCc1c[nH]cn1)C2 10.1021/jm00077a002
44273459 80702 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 482 4 0 4 3.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C=CC1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL20205 80702 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 482 4 0 4 3.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C=CC1=O)C2 10.1016/0960-894X(94)00469-V
10030575 28891 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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
ChEMBL 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 10.1021/jm00077a002
CHEMBL132210 28891 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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
ChEMBL 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 10.1021/jm00077a002
44273355 81722 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 587 8 0 6 3.9 CN(C)CCSC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
CHEMBL20319 81722 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 587 8 0 6 3.9 CN(C)CCSC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
10043741 124959 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm020133q
CHEMBL340893 124959 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm020133q
56848489 151660 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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.
ChEMBL 637 11 3 8 4.0 CCNC(=O)OCC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(C(F)(F)F)c1 nan
CHEMBL3909988 151660 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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.
ChEMBL 637 11 3 8 4.0 CCNC(=O)OCC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(C(F)(F)F)c1 nan
15307998 107874 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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)
ChEMBL 438 3 1 3 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccsc3Cc3ccccc32)cc1 10.1016/s0960-894x(99)00278-4
CHEMBL295014 107874 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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)
ChEMBL 438 3 1 3 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccsc3Cc3ccccc32)cc1 10.1016/s0960-894x(99)00278-4
10043741 124959 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
CHEMBL340893 124959 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
11158261 136428 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 692 12 1 6 8.1 CCN(CC)C1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL367323 136428 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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
ChEMBL 692 12 1 6 8.1 CCN(CC)C1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
44376291 103869 0 None - 0 Pig 8.0 pIC50 = 8.0 Binding
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
ChEMBL 1115 19 14 17 -4.8 NC(=O)CC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](N)CSSSC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1016/S0960-894X(97)00050-4
CHEMBL267405 103869 0 None - 0 Pig 8.0 pIC50 = 8.0 Binding
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
ChEMBL 1115 19 14 17 -4.8 NC(=O)CC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](N)CSSSC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1016/S0960-894X(97)00050-4
9888109 81129 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 415 2 1 5 5.1 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(Cl)c2)n1 10.1016/j.bmcl.2005.10.107
CHEMBL202447 81129 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 415 2 1 5 5.1 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(Cl)c2)n1 10.1016/j.bmcl.2005.10.107
CHEMBL2112249 216015 1 None - 2 Rat 6.0 pIC50 = 6.0 Binding
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.
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
11261339 161399 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CCC3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL399289 161399 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CCC3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
44352371 28097 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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
ChEMBL 593 9 3 7 1.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)C(N)CCS(C)(=O)=O)C2 10.1021/jm00077a002
CHEMBL131388 28097 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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
ChEMBL 593 9 3 7 1.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)C(N)CCS(C)(=O)=O)C2 10.1021/jm00077a002
10345259 123735 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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
ChEMBL 484 4 0 3 4.5 CC1CCC(=O)N1[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL338635 123735 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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
ChEMBL 484 4 0 3 4.5 CC1CCC(=O)N1[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
9887157 80717 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 399 2 1 5 4.6 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(F)c2)n1 10.1016/j.bmcl.2005.10.107
CHEMBL202106 80717 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 399 2 1 5 4.6 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(F)c2)n1 10.1016/j.bmcl.2005.10.107
10370697 125165 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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
ChEMBL 565 6 1 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CN(Cc3c[nH]cn3)C1=O)C2 10.1021/jm00077a002
CHEMBL341049 125165 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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
ChEMBL 565 6 1 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CN(Cc3c[nH]cn3)C1=O)C2 10.1021/jm00077a002
10098332 29220 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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
ChEMBL 524 6 1 5 3.6 Cn1cnc(CC(=O)N[C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)c1 10.1021/jm00077a002
CHEMBL132496 29220 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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
ChEMBL 524 6 1 5 3.6 Cn1cnc(CC(=O)N[C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)c1 10.1021/jm00077a002
10599903 21342 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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
ChEMBL 456 4 3 3 4.7 CNC(=O)NC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL120449 21342 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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
ChEMBL 456 4 3 3 4.7 CNC(=O)NC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
22405327 147054 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 409 3 0 4 5.3 O=C(c1ccc(-c2ccccc2[N+](=O)[O-])cc1)N1Cc2cccn2Cc2ccccc21 10.1016/j.bmcl.2005.08.007
CHEMBL380579 147054 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 409 3 0 4 5.3 O=C(c1ccc(-c2ccccc2[N+](=O)[O-])cc1)N1Cc2cccn2Cc2ccccc21 10.1016/j.bmcl.2005.08.007
10435004 25660 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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
ChEMBL 473 6 2 4 3.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CCN)C2 10.1021/jm00077a002
CHEMBL128328 25660 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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
ChEMBL 473 6 2 4 3.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CCN)C2 10.1021/jm00077a002
11070458 24559 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
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
ChEMBL 453 5 1 3 5.4 CC(C)NC(=O)C[C@@H]1CCCN(C(=O)c2ccc(N3CCCC3)cc2Cl)c2ccccc21 10.1021/jm020133q
CHEMBL125878 24559 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
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
ChEMBL 453 5 1 3 5.4 CC(C)NC(=O)C[C@@H]1CCCN(C(=O)c2ccc(N3CCCC3)cc2Cl)c2ccccc21 10.1021/jm020133q
10642000 121169 9 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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
ChEMBL 356 3 1 2 4.5 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccccc1 10.1021/jm960133o
CHEMBL333139 121169 9 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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
ChEMBL 356 3 1 2 4.5 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccccc1 10.1021/jm960133o
71457081 89150 0 None 64 3 Human 8.9 pKd = 8.9 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1309 24 5 14 10.2 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
71482251 89150 0 None 64 3 Human 8.9 pKd = 8.9 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1309 24 5 14 10.2 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
CHEMBL2172289 89150 0 None 64 3 Human 8.9 pKd = 8.9 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1309 24 5 14 10.2 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
44386183 162873 0 None - 1 Bovine 8.9 pKd = 8.9 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1013 18 12 14 -3.5 CC(C)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00151a016
CHEMBL406303 162873 0 None - 1 Bovine 8.9 pKd = 8.9 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1013 18 12 14 -3.5 CC(C)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00151a016
2168 10748 38 None -4 9 Rat 8.8 pKd = 8.8 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL None None None None 10.1016/s0960-894x(99)00041-4
2810 10748 38 None -4 9 Rat 8.8 pKd = 8.8 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL None None None None 10.1016/s0960-894x(99)00041-4
644077 10748 38 None -4 9 Rat 8.8 pKd = 8.8 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL None None None None 10.1016/s0960-894x(99)00041-4
CHEMBL373742 10748 38 None -4 9 Rat 8.8 pKd = 8.8 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL None None None None 10.1016/s0960-894x(99)00041-4
DB00067 10748 38 None -4 9 Rat 8.8 pKd = 8.8 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL None None None None 10.1016/s0960-894x(99)00041-4
2168 10748 38 None -7 9 Bovine 8.8 pKd = 8.8 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL None None None None 10.1021/jm00028a008
2810 10748 38 None -7 9 Bovine 8.8 pKd = 8.8 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL None None None None 10.1021/jm00028a008
644077 10748 38 None -7 9 Bovine 8.8 pKd = 8.8 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL None None None None 10.1021/jm00028a008
CHEMBL373742 10748 38 None -7 9 Bovine 8.8 pKd = 8.8 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL None None None None 10.1021/jm00028a008
DB00067 10748 38 None -7 9 Bovine 8.8 pKd = 8.8 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL None None None None 10.1021/jm00028a008
CHEMBL265119 217415 0 None - 1 Bovine 8.0 pKd = 8 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL None None None CN(CC(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=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 10.1021/jm00151a016
71461726 86467 0 None -257 2 Pig 7.0 pKd = 7 Binding
Binding affinity towards Vasopressin V2 receptor in LLCPK cellsBinding affinity towards Vasopressin V2 receptor in LLCPK cells
ChEMBL 1186 20 11 15 0.9 COc1ccc(C[C@@H]2NC(=O)C3(CCCC3)CSSC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00079a020
CHEMBL2115369 86467 0 None -257 2 Pig 7.0 pKd = 7 Binding
Binding affinity towards Vasopressin V2 receptor in LLCPK cellsBinding affinity towards Vasopressin V2 receptor in LLCPK cells
ChEMBL 1186 20 11 15 0.9 COc1ccc(C[C@@H]2NC(=O)C3(CCCC3)CSSC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00079a020
118718752 122169 0 None -26 3 Rat 6.0 pKd = 6 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1136 18 11 14 -0.5 CCN1C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]1Cc1ccc(O)cc1 10.1021/jm00010a020
CHEMBL3350124 122169 0 None -26 3 Rat 6.0 pKd = 6 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1136 18 11 14 -0.5 CCN1C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]1Cc1ccc(O)cc1 10.1021/jm00010a020
71451749 89149 0 None 38 2 Human 8.0 pKd = 8.0 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1205 25 7 15 9.2 O=C(CCC(=O)NC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc21)NCc1cn(CCOCCOCCOCCNC(=S)Nc2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)nn1 10.1021/jm3006146
CHEMBL2172288 89149 0 None 38 2 Human 8.0 pKd = 8.0 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1205 25 7 15 9.2 O=C(CCC(=O)NC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc21)NCc1cn(CCOCCOCCOCCNC(=S)Nc2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)nn1 10.1021/jm3006146
CHEMBL413706 219861 0 None - 1 Bovine 7.0 pKd = 7.0 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL None None None C[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)N(C)C(=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 10.1021/jm00151a016
118718753 122171 0 None -43 3 Rat 5.9 pKd = 5.9 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1074 18 11 15 -1.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)N(C)C(=O)CC2(CCCCC2)SSC[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 10.1021/jm00010a020
CHEMBL3350126 122171 0 None -43 3 Rat 5.9 pKd = 5.9 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1074 18 11 15 -1.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)N(C)C(=O)CC2(CCCCC2)SSC[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 10.1021/jm00010a020
44320759 167554 0 None -8 2 Bovine 6.9 pKd = 6.9 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1036 22 12 15 -4.4 CCOc1ccc(C[C@@H]2NC(=O)CCSSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)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 10.1021/jm00028a008
CHEMBL411420 167554 0 None -8 2 Bovine 6.9 pKd = 6.9 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1036 22 12 15 -4.4 CCOc1ccc(C[C@@H]2NC(=O)CCSSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)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 10.1021/jm00028a008
136961687 125370 0 None -77 3 Human 6.9 pKd = 6.9 Binding
Binding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assayBinding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 1053 21 7 12 6.4 O=C(CCCCCNC(=O)c1ccc(-c2c3ccc(=O)cc-3oc3cc(O)ccc23)c(C(=O)O)c1)NCCNC(=O)CCc1ccc(S(=O)(=O)N(CC(=O)N/N=C2\C(=O)Nc3ccccc32)c2ccc(Cl)cc2)cc1 10.1021/jm501395b
CHEMBL3416749 125370 0 None -77 3 Human 6.9 pKd = 6.9 Binding
Binding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assayBinding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 1053 21 7 12 6.4 O=C(CCCCCNC(=O)c1ccc(-c2c3ccc(=O)cc-3oc3cc(O)ccc23)c(C(=O)O)c1)NCCNC(=O)CCc1ccc(S(=O)(=O)N(CC(=O)N/N=C2\C(=O)Nc3ccccc32)c2ccc(Cl)cc2)cc1 10.1021/jm501395b
CHEMBL2370617 216666 0 None -3 3 Rat 7.8 pKd = 7.8 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL None None None CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00010a020
56678404 70104 0 None 1 2 Bovine 6.7 pKd = 6.7 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1060 20 12 14 -3.1 CC[C@H](C)[C@@H]1NC(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm00028a008
CHEMBL1793955 70104 0 None 1 2 Bovine 6.7 pKd = 6.7 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1060 20 12 14 -3.1 CC[C@H](C)[C@@H]1NC(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm00028a008
71455302 89151 0 None 234 3 Human 8.6 pKd = 8.6 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1441 33 5 17 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
71482380 89151 0 None 234 3 Human 8.6 pKd = 8.6 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1441 33 5 17 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
CHEMBL2172290 89151 0 None 234 3 Human 8.6 pKd = 8.6 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1441 33 5 17 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
71462477 89152 0 None - 1 Human 8.6 pKd = 8.6 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1573 42 5 20 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
71482382 89152 0 None - 1 Human 8.6 pKd = 8.6 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1573 42 5 20 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
CHEMBL2172291 89152 0 None - 1 Human 8.6 pKd = 8.6 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1573 42 5 20 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
CHEMBL269715 217581 0 None - 1 Bovine 7.7 pKd = 7.7 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL None None None C[C@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)N(C)C(=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 10.1021/jm00151a016
70693557 85131 0 None -6 2 Rat 5.6 pKd = 5.6 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1018 18 12 14 -4.5 CC[C@H](C)[C@H]1NC(=O)[C@@]2(CCc3ccccc3C2)NC(=O)CCSSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1016/s0960-894x(99)00041-4
CHEMBL2110163 85131 0 None -6 2 Rat 5.6 pKd = 5.6 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1018 18 12 14 -4.5 CC[C@H](C)[C@H]1NC(=O)[C@@]2(CCc3ccccc3C2)NC(=O)CCSSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1016/s0960-894x(99)00041-4
44320761 148245 0 None -1 2 Bovine 6.6 pKd = 6.6 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1110 20 13 15 -3.2 CN(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSC2(CCCCC2)CC(=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 10.1021/jm00028a008
CHEMBL384292 148245 0 None -1 2 Bovine 6.6 pKd = 6.6 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1110 20 13 15 -3.2 CN(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSC2(CCCCC2)CC(=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 10.1021/jm00028a008
44321207 103619 0 None - 1 Bovine 6.6 pKd = 6.6 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1110 20 13 15 -3.2 CN(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@H]1CSSC2(CCCCC2)CC(=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 10.1021/jm00028a008
CHEMBL265264 103619 0 None - 1 Bovine 6.6 pKd = 6.6 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1110 20 13 15 -3.2 CN(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@H]1CSSC2(CCCCC2)CC(=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 10.1021/jm00028a008
CHEMBL2370976 216751 10 None -3 3 Rat 7.6 pKd = 7.6 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL None None None CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00010a020
118718751 122168 0 None -213 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1151 19 12 15 -2.3 CN1C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]1Cc1ccc(O)cc1 10.1021/jm00010a020
CHEMBL3350123 122168 0 None -213 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1151 19 12 15 -2.3 CN1C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]1Cc1ccc(O)cc1 10.1021/jm00010a020
44320718 175673 0 None -1 2 Bovine 7.5 pKd = 7.5 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1139 22 12 15 -2.5 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00028a008
CHEMBL438387 175673 0 None -1 2 Bovine 7.5 pKd = 7.5 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1139 22 12 15 -2.5 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00028a008
44373714 103493 0 None 1 2 Rat 8.5 pKd = 8.5 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1148 32 14 16 -3.1 CC[C@H](C)[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc(=O)oc2cc(OC)ccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(=O)O 10.1016/s0960-894x(99)00041-4
CHEMBL264208 103493 0 None 1 2 Rat 8.5 pKd = 8.5 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1148 32 14 16 -3.1 CC[C@H](C)[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc(=O)oc2cc(OC)ccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(=O)O 10.1016/s0960-894x(99)00041-4
136961688 125371 0 None -21 3 Human 7.5 pKd = 7.5 Binding
Binding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assayBinding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 1206 23 5 13 7.4 CCN1/C(=C\C=C\C=C\C2=[N+](CC)c3cc(S(=O)(=O)[O-])ccc3C2(C)C)C(C)(CCCC(=O)NCCNC(=O)CCc2ccc(S(=O)(=O)N(CC(=O)N/N=C3\C(=O)Nc4ccccc43)c3ccc(Cl)cc3)cc2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm501395b
CHEMBL3416750 125371 0 None -21 3 Human 7.5 pKd = 7.5 Binding
Binding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assayBinding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 1206 23 5 13 7.4 CCN1/C(=C\C=C\C=C\C2=[N+](CC)c3cc(S(=O)(=O)[O-])ccc3C2(C)C)C(C)(CCCC(=O)NCCNC(=O)CCc2ccc(S(=O)(=O)N(CC(=O)N/N=C3\C(=O)Nc4ccccc43)c3ccc(Cl)cc3)cc2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm501395b
44321133 168614 0 None -38 2 Bovine 6.5 pKd = 6.5 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1060 20 12 14 -3.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CC2(CCCCC2)SSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm00028a008
CHEMBL414582 168614 0 None -38 2 Bovine 6.5 pKd = 6.5 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1060 20 12 14 -3.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CC2(CCCCC2)SSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm00028a008
118718383 122123 0 None -173 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1000 14 11 13 0.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2cc3ccccc3[nH]2)NC(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm00010a020
CHEMBL3349464 122123 0 None -173 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1000 14 11 13 0.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2cc3ccccc3[nH]2)NC(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm00010a020
118718384 122124 0 None -154 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1154 18 12 16 -0.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)N(C)C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm00010a020
CHEMBL3349465 122124 0 None -154 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1154 18 12 16 -0.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)N(C)C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm00010a020
10463677 122127 1 None -363 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 991 15 10 14 -0.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm00010a020
CHEMBL3349468 122127 1 None -363 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 991 15 10 14 -0.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm00010a020
44386245 175584 0 None - 1 Bovine 7.5 pKd = 7.5 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1027 18 12 14 -3.1 CC(C)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(C)[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00151a016
CHEMBL437631 175584 0 None - 1 Bovine 7.5 pKd = 7.5 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1027 18 12 14 -3.1 CC(C)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(C)[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00151a016
44321188 168685 0 None -1 2 Bovine 7.5 pKd = 7.5 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1105 22 12 15 -2.7 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)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 10.1021/jm00028a008
CHEMBL415230 168685 0 None -1 2 Bovine 7.5 pKd = 7.5 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1105 22 12 15 -2.7 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)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 10.1021/jm00028a008
145947801 174492 0 None -190 2 Human 6.5 pKd = 6.5 Binding
Binding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assayBinding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 1381 42 2 22 7.7 CCN1/C(=C\C=C\C=C\C2=[N+](CC)c3cc(S(=O)(=O)[O-])ccc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCc2nnc(N3CC(Oc4ccc(F)cc4Cl)C3)n2-c2ccc(OC)nc2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm501395b
CHEMBL3416754 174492 0 None -190 2 Human 6.5 pKd = 6.5 Binding
Binding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assayBinding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 1381 42 2 22 7.7 CCN1/C(=C\C=C\C=C\C2=[N+](CC)c3cc(S(=O)(=O)[O-])ccc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCc2nnc(N3CC(Oc4ccc(F)cc4Cl)C3)n2-c2ccc(OC)nc2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm501395b
CHEMBL4302530 174492 0 None -190 2 Human 6.5 pKd = 6.5 Binding
Binding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assayBinding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 1381 42 2 22 7.7 CCN1/C(=C\C=C\C=C\C2=[N+](CC)c3cc(S(=O)(=O)[O-])ccc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCc2nnc(N3CC(Oc4ccc(F)cc4Cl)C3)n2-c2ccc(OC)nc2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm501395b
118718386 122126 0 None -186 3 Rat 5.4 pKd = 5.4 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 991 14 10 14 -0.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)N(C)C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm00010a020
CHEMBL3349467 122126 0 None -186 3 Rat 5.4 pKd = 5.4 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 991 14 10 14 -0.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)N(C)C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm00010a020
44373744 57947 0 None -52 2 Rat 6.4 pKd = 6.4 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 993 20 12 14 -4.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCC(N)=O)NC1=O 10.1016/s0960-894x(99)00041-4
CHEMBL157988 57947 0 None -52 2 Rat 6.4 pKd = 6.4 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 993 20 12 14 -4.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCC(N)=O)NC1=O 10.1016/s0960-894x(99)00041-4
44320760 213164 0 None -52 2 Bovine 6.4 pKd = 6.4 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 992 20 12 14 -4.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm00028a008
CHEMBL87636 213164 0 None -52 2 Bovine 6.4 pKd = 6.4 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 992 20 12 14 -4.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm00028a008
CHEMBL410025 219575 0 None - 1 Bovine 7.4 pKd = 7.4 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL None None None CN(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=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 10.1021/jm00151a016
118718749 122166 0 None -5 3 Rat 7.3 pKd = 7.3 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1136 18 11 14 -0.5 CCN1C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]1Cc1ccc(O)cc1 10.1021/jm00010a020
CHEMBL3350119 122166 0 None -5 3 Rat 7.3 pKd = 7.3 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1136 18 11 14 -0.5 CCN1C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]1Cc1ccc(O)cc1 10.1021/jm00010a020
44373715 162480 0 None -131 2 Rat 5.3 pKd = 5.3 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1031 20 13 14 -4.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)CCSSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCC(N)=O)NC1=O 10.1016/s0960-894x(99)00041-4
CHEMBL405165 162480 0 None -131 2 Rat 5.3 pKd = 5.3 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1031 20 13 14 -4.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)CCSSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCC(N)=O)NC1=O 10.1016/s0960-894x(99)00041-4
145947419 174436 0 None -323 2 Human 6.3 pKd = 6.3 Binding
Binding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assayBinding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 1204 30 2 18 7.6 CCN1/C(=C\C=C\C=C\C2=[N+](CC)c3cc(S(=O)(=O)[O-])ccc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCc2nnc(N3CC(Oc4ccc(F)cc4Cl)C3)n2-c2ccc(OC)nc2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm501395b
CHEMBL3416753 174436 0 None -323 2 Human 6.3 pKd = 6.3 Binding
Binding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assayBinding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 1204 30 2 18 7.6 CCN1/C(=C\C=C\C=C\C2=[N+](CC)c3cc(S(=O)(=O)[O-])ccc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCc2nnc(N3CC(Oc4ccc(F)cc4Cl)C3)n2-c2ccc(OC)nc2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm501395b
CHEMBL4301807 174436 0 None -323 2 Human 6.3 pKd = 6.3 Binding
Binding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assayBinding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 1204 30 2 18 7.6 CCN1/C(=C\C=C\C=C\C2=[N+](CC)c3cc(S(=O)(=O)[O-])ccc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCc2nnc(N3CC(Oc4ccc(F)cc4Cl)C3)n2-c2ccc(OC)nc2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm501395b
44385836 167477 0 None - 1 Bovine 7.3 pKd = 7.3 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1056 20 13 15 -4.5 C[C@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)N(C)C(=O)[C@@H]1CSSCCC(=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 10.1021/jm00151a016
CHEMBL411357 167477 0 None - 1 Bovine 7.3 pKd = 7.3 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1056 20 13 15 -4.5 C[C@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)N(C)C(=O)[C@@H]1CSSCCC(=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 10.1021/jm00151a016
70693566 85145 0 None -2 2 Rat 5.3 pKd = 5.3 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1018 18 12 14 -4.5 CC[C@H](C)[C@H]1NC(=O)[C@]2(CCc3ccccc3C2)NC(=O)CCSSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1016/s0960-894x(99)00041-4
CHEMBL2110297 85145 0 None -2 2 Rat 5.3 pKd = 5.3 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1018 18 12 14 -4.5 CC[C@H](C)[C@H]1NC(=O)[C@]2(CCc3ccccc3C2)NC(=O)CCSSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1016/s0960-894x(99)00041-4
10011419 122170 0 None -2 3 Rat 7.3 pKd = 7.3 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1092 17 11 13 -1.0 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00010a020
CHEMBL3350125 122170 0 None -2 3 Rat 7.3 pKd = 7.3 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1092 17 11 13 -1.0 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00010a020
44294474 103787 0 None 1 3 Rat 8.1 pKd = 8.1 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1092 17 11 13 -1.0 CC(C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm00010a020
CHEMBL266643 103787 0 None 1 3 Rat 8.1 pKd = 8.1 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1092 17 11 13 -1.0 CC(C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm00010a020
44386247 168463 0 None - 1 Bovine 8.1 pKd = 8.1 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1042 20 13 15 -4.9 CN(CC(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSCCC(=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 10.1021/jm00151a016
CHEMBL413249 168463 0 None - 1 Bovine 8.1 pKd = 8.1 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1042 20 13 15 -4.9 CN(CC(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSCCC(=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 10.1021/jm00151a016
44321134 119339 0 None -45 2 Bovine 6.1 pKd = 6.1 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 963 16 9 14 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCSSC[C@H](C(=O)N2CCC[C@H]2C(=O)N(C)CC(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm00028a008
CHEMBL330022 119339 0 None -45 2 Bovine 6.1 pKd = 6.1 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 963 16 9 14 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCSSC[C@H](C(=O)N2CCC[C@H]2C(=O)N(C)CC(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm00028a008
CHEMBL217517 216155 0 None - 1 Bovine 8.0 pKd = 8.0 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00151a016
CHEMBL2371674 216886 0 None - 1 Bovine 8.0 pKd = 8.0 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(C)[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00151a016
44321206 103578 0 None -13 2 Bovine 7.0 pKd = 7.0 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1094 20 12 14 -2.9 CN(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSC2(CCCCC2)CC(=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 10.1021/jm00028a008
CHEMBL265017 103578 0 None -13 2 Bovine 7.0 pKd = 7.0 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1094 20 12 14 -2.9 CN(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSC2(CCCCC2)CC(=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 10.1021/jm00028a008
44419039 144174 0 None -1 8 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1096 20 14 15 -4.6 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm060928n
CHEMBL375324 144174 0 None -1 8 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1096 20 14 15 -4.6 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm060928n
44419026 175278 17 None 1230 2 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 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 10.1021/jm060928n
CHEMBL435323 175278 17 None 1230 2 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 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 10.1021/jm060928n
2181 8113 42 None 6 7 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL None None None None 10.1021/jm060928n
2182 8113 42 None 6 7 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL None None None None 10.1021/jm060928n
27991 8113 42 None 6 7 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL None None None None 10.1021/jm060928n
5311065 8113 42 None 6 7 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL None None None None 10.1021/jm060928n
CHEMBL1429 8113 42 None 6 7 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL None None None None 10.1021/jm060928n
CHEMBL264448 8113 42 None 6 7 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL None None None None 10.1021/jm060928n
DB00035 8113 42 None 6 7 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL None None None None 10.1021/jm060928n
44419025 91071 0 None -1 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 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 10.1021/jm060928n
CHEMBL221436 91071 0 None -1 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 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 10.1021/jm060928n
151171 7947 50 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
216322 7947 50 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
2203 7947 50 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
732 7947 50 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
CHEMBL1755 7947 50 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
DB00872 7947 50 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
44520886 195598 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]vasopressin from rat vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from rat vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 628 7 2 4 7.4 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL506235 195598 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]vasopressin from rat vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from rat vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 628 7 2 4 7.4 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
216237 10615 89 None 2 5 Human 9.4 pKi = 9.4 Binding
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%
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/jm000108p
2226 10615 89 None 2 5 Human 9.4 pKi = 9.4 Binding
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%
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/jm000108p
4110 10615 89 None 2 5 Human 9.4 pKi = 9.4 Binding
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%
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/jm000108p
443894 10615 89 None 2 5 Human 9.4 pKi = 9.4 Binding
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%
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/jm000108p
CHEMBL344159 10615 89 None 2 5 Human 9.4 pKi = 9.4 Binding
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%
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/jm000108p
DB06212 10615 89 None 2 5 Human 9.4 pKi = 9.4 Binding
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%
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/jm000108p
2168 10748 38 None -4 9 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL None None None None 10.1021/jm060928n
2810 10748 38 None -4 9 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL None None None None 10.1021/jm060928n
644077 10748 38 None -4 9 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL None None None None 10.1021/jm060928n
CHEMBL373742 10748 38 None -4 9 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL None None None None 10.1021/jm060928n
DB00067 10748 38 None -4 9 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL None None None None 10.1021/jm060928n
CHEMBL2371605 216884 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL None None None CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
10411308 208013 0 None 2 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.8b00697
CHEMBL603708 208013 0 None 2 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.8b00697
10411308 208013 0 None 2 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm3006146
CHEMBL603708 208013 0 None 2 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm3006146
10411308 208013 0 None 2 3 Human 9.2 pKi = 9.2 Binding
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
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm901084f
CHEMBL603708 208013 0 None 2 3 Human 9.2 pKi = 9.2 Binding
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
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm901084f
135413562 8986 15 None -1 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 624 14 3 7 1.1 CN(CCCNC(=O)CCc1ccc(cc1)S(=O)(=O)N(c1ccc(cc1)Cl)CC(=O)NNC1=c2ccccc2=NC1=O)C 10.1021/jm901812z
2194 8986 15 None -1 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 624 14 3 7 1.1 CN(CCCNC(=O)CCc1ccc(cc1)S(=O)(=O)N(c1ccc(cc1)Cl)CC(=O)NNC1=c2ccccc2=NC1=O)C 10.1021/jm901812z
CHEMBL445816 8986 15 None -1 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 624 14 3 7 1.1 CN(CCCNC(=O)CCc1ccc(cc1)S(=O)(=O)N(c1ccc(cc1)Cl)CC(=O)NNC1=c2ccccc2=NC1=O)C 10.1021/jm901812z
CHEMBL2371604 216883 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL None None None CCOc1ccc(C[C@@H]2NC(=O)CC3(CCC(C)CC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
2205 10895 6 None -3 5 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 10.1021/jm010544r
9810140 10895 6 None -3 5 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 10.1021/jm010544r
CHEMBL307483 10895 6 None -3 5 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 10.1021/jm010544r
16051933 144908 4 None -3 8 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=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 10.1021/jm060928n
CHEMBL376685 144908 4 None -3 8 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=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 10.1021/jm060928n
DB00035 144908 4 None -3 8 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=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 10.1021/jm060928n
71462477 89152 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assayDisplacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assay
ChEMBL 1573 42 5 20 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
71482382 89152 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assayDisplacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assay
ChEMBL 1573 42 5 20 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
CHEMBL2172291 89152 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assayDisplacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assay
ChEMBL 1573 42 5 20 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
2198 10193 2 None 46 2 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 Clc1cc(ccc1C(=O)N1C[C@H]2COCCN2Cc2c1cccc2)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2004.03.083
9807249 10193 2 None 46 2 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 Clc1cc(ccc1C(=O)N1C[C@H]2COCCN2Cc2c1cccc2)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL1192593 10193 2 None 46 2 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 Clc1cc(ccc1C(=O)N1C[C@H]2COCCN2Cc2c1cccc2)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2004.03.083
44382498 103268 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1093 17 10 13 0.6 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCC(C)CC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
CHEMBL262482 103268 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1093 17 10 13 0.6 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCC(C)CC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
44375638 175627 0 None 6 2 Human 9.0 pKi = 9 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
CHEMBL438014 175627 0 None 6 2 Human 9.0 pKi = 9 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
CHEMBL3084974 217765 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL None None None CCOc1ccc(C[C@@H]2NC(=O)CC3(CCC(C)CC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
216237 10615 89 None 2 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.1c00863
2226 10615 89 None 2 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.1c00863
4110 10615 89 None 2 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.1c00863
443894 10615 89 None 2 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.1c00863
CHEMBL344159 10615 89 None 2 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.1c00863
DB06212 10615 89 None 2 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.1c00863
44382370 148328 0 None 3 2 Human 9.0 pKi = 9.0 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
CHEMBL384776 148328 0 None 3 2 Human 9.0 pKi = 9.0 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
2205 10895 6 None -3 5 Human 8.9 pKi = 8.9 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 10.1021/jm010544r
9810140 10895 6 None -3 5 Human 8.9 pKi = 8.9 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 10.1021/jm010544r
CHEMBL307483 10895 6 None -3 5 Human 8.9 pKi = 8.9 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 10.1021/jm010544r
2205 10895 6 None -3 5 Rat 8.9 pKi = 8.9 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 10.1016/s0960-894x(01)00723-5
9810140 10895 6 None -3 5 Rat 8.9 pKi = 8.9 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 10.1016/s0960-894x(01)00723-5
CHEMBL307483 10895 6 None -3 5 Rat 8.9 pKi = 8.9 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 10.1016/s0960-894x(01)00723-5
44419025 91071 0 None -4 8 Human 8.9 pKi = 8.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 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 10.1021/jm030611c
CHEMBL221436 91071 0 None -4 8 Human 8.9 pKi = 8.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 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 10.1021/jm030611c
2168 10748 38 None -15 9 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL None None None None 10.1021/jm1016208
2810 10748 38 None -15 9 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL None None None None 10.1021/jm1016208
644077 10748 38 None -15 9 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL None None None None 10.1021/jm1016208
CHEMBL373742 10748 38 None -15 9 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL None None None None 10.1021/jm1016208
DB00067 10748 38 None -15 9 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL None None None None 10.1021/jm1016208
CHEMBL408474 219494 0 None - 1 Pig 8.9 pKi = 8.9 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL None None None NCCCC[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(=O)O 10.1021/jm00150a003
2168 10748 38 None -15 9 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assayDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assay
ChEMBL None None None None 10.1021/jm3006146
2810 10748 38 None -15 9 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assayDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assay
ChEMBL None None None None 10.1021/jm3006146
644077 10748 38 None -15 9 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assayDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assay
ChEMBL None None None None 10.1021/jm3006146
CHEMBL373742 10748 38 None -15 9 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assayDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assay
ChEMBL None None None None 10.1021/jm3006146
DB00067 10748 38 None -15 9 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assayDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assay
ChEMBL None None None None 10.1021/jm3006146
44325703 118180 0 None 75 2 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccc(O)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL327242 118180 0 None 75 2 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccc(O)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
2168 10748 38 None -15 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL None None None None 10.1021/jm3006146
2810 10748 38 None -15 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL None None None None 10.1021/jm3006146
644077 10748 38 None -15 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL None None None None 10.1021/jm3006146
CHEMBL373742 10748 38 None -15 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL None None None None 10.1021/jm3006146
DB00067 10748 38 None -15 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL None None None None 10.1021/jm3006146
CHEMBL2369831 216477 1 None -1 4 Human 8.8 pKi = 8.8 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None C[C@@H](O)[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](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
44351500 124255 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidney
ChEMBL 995 16 10 12 0.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL339943 124255 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidney
ChEMBL 995 16 10 12 0.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44297505 172636 0 None -7 3 Rat 8.8 pKi = 8.8 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1329 38 15 16 -1.8 CN(C(=O)CCc1ccc(N=[N+]=[N-])cc1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
CHEMBL424905 172636 0 None -7 3 Rat 8.8 pKi = 8.8 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1329 38 15 16 -1.8 CN(C(=O)CCc1ccc(N=[N+]=[N-])cc1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
216237 10615 89 None 2 5 Human 8.8 pKi = 8.8 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
2226 10615 89 None 2 5 Human 8.8 pKi = 8.8 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
4110 10615 89 None 2 5 Human 8.8 pKi = 8.8 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
443894 10615 89 None 2 5 Human 8.8 pKi = 8.8 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
CHEMBL344159 10615 89 None 2 5 Human 8.8 pKi = 8.8 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
DB06212 10615 89 None 2 5 Human 8.8 pKi = 8.8 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
16109443 148497 0 None -9 4 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1040 18 14 15 -4.0 N=C(N)NCCC[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](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL385739 148497 0 None -9 4 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1040 18 14 15 -4.0 N=C(N)NCCC[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](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
44325362 214123 0 None 354 2 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccc(F)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL93603 214123 0 None 354 2 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccc(F)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
71455302 89151 0 None 234 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assayDisplacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assay
ChEMBL 1441 33 5 17 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
71482380 89151 0 None 234 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assayDisplacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assay
ChEMBL 1441 33 5 17 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
CHEMBL2172290 89151 0 None 234 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assayDisplacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assay
ChEMBL 1441 33 5 17 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
44520857 186241 0 None 3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 562 5 2 6 5.2 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccc(N)n4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL474072 186241 0 None 3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 562 5 2 6 5.2 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccc(N)n4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
167184780 197960 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 566 8 2 4 7.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCc3ccncc3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5189068 197960 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 566 8 2 4 7.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCc3ccncc3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
168295452 199149 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 560 10 1 4 7.2 CCN(CC)CCCN1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc21 10.1021/acs.jmedchem.2c00567
CHEMBL5207405 199149 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 560 10 1 4 7.2 CCN(CC)CCCN1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc21 10.1021/acs.jmedchem.2c00567
CHEMBL2370641 216683 0 None -1 2 Pig 8.0 pKi = 8 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL None None None CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)NCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL2371440 216825 0 None - 1 Pig 8.0 pKi = 8 Binding
Inhibition of LVP-sensitive adenylate cyclase in a pig renal medullary preparationInhibition of LVP-sensitive adenylate cyclase in a pig renal medullary preparation
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00399a009
44325732 172205 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 533 4 1 4 6.5 Cc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CC2CSCCN2Cc2ccccc21 10.1016/j.bmcl.2004.03.083
CHEMBL423868 172205 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 533 4 1 4 6.5 Cc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CC2CSCCN2Cc2ccccc21 10.1016/j.bmcl.2004.03.083
44325543 214064 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 1 4 6.8 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3cccc(Cl)c32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL93195 214064 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 1 4 6.8 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3cccc(Cl)c32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325731 214067 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(F)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL93205 214067 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(F)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44297449 176039 0 None -22 3 Rat 8.0 pKi = 8 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1315 37 15 16 -2.2 CN(C(=O)Cc1cccc(N=[N+]=[N-])c1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
CHEMBL441195 176039 0 None -22 3 Rat 8.0 pKi = 8 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1315 37 15 16 -2.2 CN(C(=O)Cc1cccc(N=[N+]=[N-])c1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
145976546 170419 0 None 7 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 381 2 1 4 4.3 Cc1ccn(-c2ccc(C(=O)N3CCCC(O)c4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL4204008 170419 0 None 7 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 381 2 1 4 4.3 Cc1ccn(-c2ccc(C(=O)N3CCCC(O)c4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
44419030 168393 19 None -630 4 Rat 7.0 pKi = 7 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1025 18 11 14 -1.5 CC(C)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](CCCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL412972 168393 19 None -630 4 Rat 7.0 pKi = 7 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1025 18 11 14 -1.5 CC(C)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](CCCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
10303620 213055 0 None -954 4 Rat 6.0 pKi = 6 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 577 12 0 6 7.8 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCC(N2CCCCC2)CC1 10.1021/jm010544r
CHEMBL86949 213055 0 None -954 4 Rat 6.0 pKi = 6 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 577 12 0 6 7.8 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCC(N2CCCCC2)CC1 10.1021/jm010544r
11092056 113815 0 None -354 2 Human 5.0 pKi = 5.0 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 481 9 0 6 5.3 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCN1CCN(C)CC1 10.1021/jm010544r
CHEMBL315524 113815 0 None -354 2 Human 5.0 pKi = 5.0 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 481 9 0 6 5.3 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCN1CCN(C)CC1 10.1021/jm010544r
44321415 119092 0 None -269 2 Human 5.0 pKi = 5.0 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 467 8 0 6 4.9 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCN1CCN(C)CC1 10.1021/jm010544r
CHEMBL329209 119092 0 None -269 2 Human 5.0 pKi = 5.0 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 467 8 0 6 4.9 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCN1CCN(C)CC1 10.1021/jm010544r
46890484 13801 0 None -93 2 Human 6.0 pKi = 6.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 381 2 0 1 6.4 Cc1ccccc1-c1ccc(C(=O)N2C[C@@]3(C)C[C@@H]2CC(C)(C)C3)c(Cl)c1 10.1016/j.bmcl.2010.04.068
CHEMBL1084822 13801 0 None -93 2 Human 6.0 pKi = 6.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 381 2 0 1 6.4 Cc1ccccc1-c1ccc(C(=O)N2C[C@@]3(C)C[C@@H]2CC(C)(C)C3)c(Cl)c1 10.1016/j.bmcl.2010.04.068
16109439 144020 0 None -104 5 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1023 15 11 14 -1.7 NC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
CHEMBL375187 144020 0 None -104 5 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1023 15 11 14 -1.7 NC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
46890486 13803 0 None -28 2 Human 6.0 pKi = 6.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 361 2 0 1 6.0 Cc1ccccc1-c1ccc(C(=O)N2C[C@@]3(C)C[C@@H]2CC(C)(C)C3)cc1C 10.1016/j.bmcl.2010.04.068
CHEMBL1084824 13803 0 None -28 2 Human 6.0 pKi = 6.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 361 2 0 1 6.0 Cc1ccccc1-c1ccc(C(=O)N2C[C@@]3(C)C[C@@H]2CC(C)(C)C3)cc1C 10.1016/j.bmcl.2010.04.068
CHEMBL2369847 216488 0 None -112 4 Human 6.0 pKi = 6.0 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
46890528 13804 0 None -199 2 Human 7.0 pKi = 7.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 411 3 0 2 6.4 COc1cc(-c2ccccc2C)c(Cl)cc1C(=O)N1C[C@]2(C)C[C@H]1CC(C)(C)C2 10.1016/j.bmcl.2010.04.068
CHEMBL1084825 13804 0 None -199 2 Human 7.0 pKi = 7.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 411 3 0 2 6.4 COc1cc(-c2ccccc2C)c(Cl)cc1C(=O)N1C[C@]2(C)C[C@H]1CC(C)(C)C2 10.1016/j.bmcl.2010.04.068
168294940 199166 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 576 7 1 5 5.3 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1Br 10.1021/acs.jmedchem.2c00567
CHEMBL5207597 199166 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 576 7 1 5 5.3 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1Br 10.1021/acs.jmedchem.2c00567
CHEMBL5081323 221522 0 None -2691 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL None None None Cc1ccc2c(c1)CC(O)Cc1nnc([C@H]3CC[C@H](Oc4ccccn4)CC3)n1-2 10.1021/acs.jmedchem.1c00863
CHEMBL2369835 216479 0 None -7 4 Human 6.0 pKi = 6.0 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
44520864 179416 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 603 5 1 6 6.8 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4nc5ccccc5s4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL449517 179416 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 603 5 1 6 6.8 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4nc5ccccc5s4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44520858 181197 0 None 4 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 590 6 1 6 5.7 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccc(N(C)C)n4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL455279 181197 0 None 4 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 590 6 1 6 5.7 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccc(N(C)C)n4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44520863 188635 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 553 5 1 6 5.7 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4nccs4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL477868 188635 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 553 5 1 6 5.7 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4nccs4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44520862 196385 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 548 5 1 6 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccncn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL514772 196385 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 548 5 1 6 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccncn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44520871 199392 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 513 5 2 5 3.5 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCC(N)=O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL521597 199392 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 513 5 2 5 3.5 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCC(N)=O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44520875 19246 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 609 6 1 5 7.0 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3ccc(-c4ccccc4)n3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1186237 19246 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 609 6 1 5 7.0 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3ccc(-c4ccccc4)n3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL455418 19246 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 609 6 1 5 7.0 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3ccc(-c4ccccc4)n3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
44520883 19467 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 564 5 1 4 6.5 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1187505 19467 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 564 5 1 4 6.5 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL505517 19467 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 564 5 1 4 6.5 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
164946750 196905 1 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 574 8 2 5 6.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5173331 196905 1 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 574 8 2 5 6.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
44351384 123775 0 None - 1 Pig 8.0 pKi = 8.0 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 980 18 10 13 2.2 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)NCCCCCNC(N)C=N)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL338798 123775 0 None - 1 Pig 8.0 pKi = 8.0 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 980 18 10 13 2.2 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)NCCCCCNC(N)C=N)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44351279 168222 0 None - 1 Pig 8.0 pKi = 8.0 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 1055 14 8 12 3.1 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCc3cccc(CN)c3)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL412732 168222 0 None - 1 Pig 8.0 pKi = 8.0 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 1055 14 8 12 3.1 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCc3cccc(CN)c3)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44325689 213639 0 None 44 2 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 1 4 6.8 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL90657 213639 0 None 44 2 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 1 4 6.8 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325505 214222 0 None 562 2 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1cc(F)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL94133 214222 0 None 562 2 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1cc(F)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL1790551 215679 0 None -229 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 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]2C[C@@H](CN(C)C)C=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
44361403 40619 1 None -457 5 Rat 5.0 pKi = 5.0 Binding
Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from ratsBinding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats
ChEMBL 491 5 0 5 4.1 CC(=O)N1CCCC(COc2ccc(C(=O)N3CCC(N4C(=O)OCc5ccccc54)CC3)cc2)C1 10.1021/jm00023a002
CHEMBL142324 40619 1 None -457 5 Rat 5.0 pKi = 5.0 Binding
Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from ratsBinding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats
ChEMBL 491 5 0 5 4.1 CC(=O)N1CCCC(COc2ccc(C(=O)N3CCC(N4C(=O)OCc5ccccc54)CC3)cc2)C1 10.1021/jm00023a002
44361387 126192 0 None -724 5 Rat 5.0 pKi = 5.0 Binding
Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from ratsBinding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats
ChEMBL 505 6 0 5 4.6 CC(=O)N1CCCCC1CCOc1ccc(C(=O)N2CCC(N3C(=O)OCc4ccccc43)CC2)cc1 10.1021/jm00023a002
CHEMBL344752 126192 0 None -724 5 Rat 5.0 pKi = 5.0 Binding
Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from ratsBinding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats
ChEMBL 505 6 0 5 4.6 CC(=O)N1CCCCC1CCOc1ccc(C(=O)N2CCC(N3C(=O)OCc4ccccc43)CC2)cc1 10.1021/jm00023a002
10863737 213409 0 None -1202 2 Human 5.0 pKi = 5.0 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 477 11 0 6 6.7 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCn1ccnc1 10.1021/jm010544r
CHEMBL89177 213409 0 None -1202 2 Human 5.0 pKi = 5.0 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 477 11 0 6 6.7 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCn1ccnc1 10.1021/jm010544r
CHEMBL2369837 216481 0 None -6165 4 Human 5.0 pKi = 5.0 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None NCCCC[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](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
11366713 144000 0 None -2511 8 Human 6.0 pKi = 6.0 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1054 19 13 15 -3.9 NCCC[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](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
CHEMBL375096 144000 0 None -2511 8 Human 6.0 pKi = 6.0 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1054 19 13 15 -3.9 NCCC[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](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
145974638 171373 0 None -7 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 347 2 1 4 3.7 Cc1ccn(-c2ccc(C(=O)N3CCCC(O)c4ccccc43)cc2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL4215696 171373 0 None -7 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 347 2 1 4 3.7 Cc1ccn(-c2ccc(C(=O)N3CCCC(O)c4ccccc43)cc2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL2369830 216476 0 None -275 4 Human 6.9 pKi = 6.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None CCCC[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](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
46890572 14130 0 None -1148 2 Human 5.9 pKi = 5.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 420 4 1 3 4.8 CNC(=O)c1cccc(-c2ccc(C(=O)N3C[C@]4(C)C[C@H]3CC(C)(C)C4)cc2OC)c1 10.1016/j.bmcl.2010.04.068
CHEMBL1086294 14130 0 None -1148 2 Human 5.9 pKi = 5.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 420 4 1 3 4.8 CNC(=O)c1cccc(-c2ccc(C(=O)N3C[C@]4(C)C[C@H]3CC(C)(C)C4)cc2OC)c1 10.1016/j.bmcl.2010.04.068
10208389 85406 0 None -8128 4 Rat 4.9 pKi = 4.9 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 523 11 0 6 6.4 Cc1cccc(OCCCCCCN2CCN(C)CC2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
CHEMBL2112339 85406 0 None -8128 4 Rat 4.9 pKi = 4.9 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 523 11 0 6 6.4 Cc1cccc(OCCCCCCN2CCN(C)CC2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
44520865 195904 0 None 6 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 586 5 2 5 6.1 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4nc5ccccc5[nH]4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL510500 195904 0 None 6 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 586 5 2 5 6.1 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4nc5ccccc5[nH]4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
167183380 197353 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 587 8 2 5 5.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCN(C)CC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5180200 197353 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 587 8 2 5 5.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCN(C)CC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
10674616 198214 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 572 8 1 4 7.3 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCCCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
CHEMBL5192961 198214 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 572 8 1 4 7.3 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCCCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
168290973 198658 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 588 8 1 5 6.5 Cc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CCCN(CCCN2CCOCC2)c2ccccc21 10.1021/acs.jmedchem.2c00567
CHEMBL5199628 198658 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 588 8 1 5 6.5 Cc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CCCN(CCCN2CCOCC2)c2ccccc21 10.1021/acs.jmedchem.2c00567
44294575 88889 0 None - 1 Pig 7.9 pKi = 7.9 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL216606 88889 0 None - 1 Pig 7.9 pKi = 7.9 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
44294542 103258 0 None - 1 Pig 7.9 pKi = 7.9 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL262423 103258 0 None - 1 Pig 7.9 pKi = 7.9 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
71460754 89162 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1141 17 2 11 9.7 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)N4CCN(CCC(=O)NC5CCCN(C(=O)c6ccc(NC(=O)c7ccccc7-c7ccccc7)cc6)c6ccccc65)CC4)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2172392 89162 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1141 17 2 11 9.7 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)N4CCN(CCC(=O)NC5CCCN(C(=O)c6ccc(NC(=O)c7ccccc7-c7ccccc7)cc6)c6ccccc65)CC4)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
44419028 103684 17 None -10 8 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1093 18 12 14 -1.6 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm060928n
CHEMBL265858 103684 17 None -10 8 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1093 18 12 14 -1.6 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm060928n
10615 7360 32 None -1288249 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1021/acs.jmedchem.1c00863
46200932 7360 32 None -1288249 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1021/acs.jmedchem.1c00863
CHEMBL4297183 7360 32 None -1288249 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1021/acs.jmedchem.1c00863
DB14823 7360 32 None -1288249 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1021/acs.jmedchem.1c00863
46890529 13507 0 None -47 2 Human 5.9 pKi = 5.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 411 3 0 2 6.4 COc1cc(-c2ccccc2C)c(Cl)cc1C(=O)N1C[C@@]2(C)C[C@@H]1CC(C)(C)C2 10.1016/j.bmcl.2010.04.068
CHEMBL1083730 13507 0 None -47 2 Human 5.9 pKi = 5.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 411 3 0 2 6.4 COc1cc(-c2ccccc2C)c(Cl)cc1C(=O)N1C[C@@]2(C)C[C@@H]1CC(C)(C)C2 10.1016/j.bmcl.2010.04.068
145976648 170622 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 293 3 0 1 4.6 CCCc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/acs.jmedchem.8b00697
CHEMBL4206482 170622 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 293 3 0 1 4.6 CCCc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/acs.jmedchem.8b00697
46890152 13525 0 None -3 2 Human 6.9 pKi = 6.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 457 2 0 2 7.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3csc4ccccc34)c(Cl)c2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1083765 13525 0 None -3 2 Human 6.9 pKi = 6.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 457 2 0 2 7.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3csc4ccccc34)c(Cl)c2Cl)C1 10.1016/j.bmcl.2010.04.068
10164478 213464 0 None -1174 4 Rat 5.9 pKi = 5.9 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 509 11 0 6 6.1 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCN(C)CC1 10.1021/jm010544r
CHEMBL89552 213464 0 None -1174 4 Rat 5.9 pKi = 5.9 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 509 11 0 6 6.1 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCN(C)CC1 10.1021/jm010544r
118734336 125378 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 418 3 1 3 4.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[S@@+]([O-])c3ccccc32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416770 125378 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 418 3 1 3 4.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[S@@+]([O-])c3ccccc32)cc1 10.1021/acs.jmedchem.5b00289
11569194 78882 0 None -316 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 479 7 2 3 3.5 CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)NC(C)C)c1ccc(F)cc1 10.1021/jm901812z
CHEMBL197793 78882 0 None -316 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 479 7 2 3 3.5 CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)NC(C)C)c1ccc(F)cc1 10.1021/jm901812z
25212177 181608 10 None -2818 4 Human 4.9 pKi = 4.9 Binding
Binding affinity to vasopressin V2 receptor by filtration assayBinding affinity to vasopressin V2 receptor by filtration assay
ChEMBL 463 7 0 7 3.9 COc1ccc(N(Cc2ccc(-c3ccccc3C)cn2)S(=O)(=O)c2cn(C)c(C)n2)cn1 10.1016/j.bmcl.2008.11.018
CHEMBL456263 181608 10 None -2818 4 Human 4.9 pKi = 4.9 Binding
Binding affinity to vasopressin V2 receptor by filtration assayBinding affinity to vasopressin V2 receptor by filtration assay
ChEMBL 463 7 0 7 3.9 COc1ccc(N(Cc2ccc(-c3ccccc3C)cn2)S(=O)(=O)c2cn(C)c(C)n2)cn1 10.1016/j.bmcl.2008.11.018
44520849 208492 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 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 10.1016/j.bmc.2009.10.038
CHEMBL606464 208492 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 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 10.1016/j.bmc.2009.10.038
168289573 198618 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 572 8 2 4 7.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCCCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5198918 198618 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 572 8 2 4 7.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCCCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
168286187 198267 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 587 8 1 5 6.1 CN1CCN(CCCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccccc32)CC1 10.1021/acs.jmedchem.2c00567
CHEMBL5193621 198267 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 587 8 1 5 6.1 CN1CCN(CCCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccccc32)CC1 10.1021/acs.jmedchem.2c00567
44335329 174617 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 561 4 1 3 7.6 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(C5)N4Cc4cc(Cl)ccc43)cc2)cc1 10.1016/s0960-894x(02)00649-2
CHEMBL430841 174617 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 561 4 1 3 7.6 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(C5)N4Cc4cc(Cl)ccc43)cc2)cc1 10.1016/s0960-894x(02)00649-2
44325704 119084 0 None 64 2 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1cc(O)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL329141 119084 0 None 64 2 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1cc(O)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44316235 167207 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1011 16 12 14 -3.6 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](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm030611c
CHEMBL411148 167207 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1011 16 12 14 -3.6 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](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm030611c
9938406 100092 1 None -181 6 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Vasopressin V2 receptor by using functional assayBinding affinity towards cloned human Vasopressin V2 receptor by using functional assay
ChEMBL 589 7 0 6 4.7 CC(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)OCc5ccccc54)CC3)c(OCC(F)(F)F)c2)CC1 10.1016/s0960-894x(99)00181-x
CHEMBL24526 100092 1 None -181 6 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Vasopressin V2 receptor by using functional assayBinding affinity towards cloned human Vasopressin V2 receptor by using functional assay
ChEMBL 589 7 0 6 4.7 CC(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)OCc5ccccc54)CC3)c(OCC(F)(F)F)c2)CC1 10.1016/s0960-894x(99)00181-x
46890101 14075 0 None -181 2 Human 6.9 pKi = 6.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 414 3 0 3 6.0 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc2cccnc12 10.1016/j.bmcl.2010.04.068
CHEMBL1086070 14075 0 None -181 2 Human 6.9 pKi = 6.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 414 3 0 3 6.0 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc2cccnc12 10.1016/j.bmcl.2010.04.068
53349471 125381 0 None -22 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 413 3 1 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(C)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416774 125381 0 None -22 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 413 3 1 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(C)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
44351328 26164 0 None - 1 Pig 6.9 pKi = 6.9 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 909 10 7 11 2.3 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL129274 26164 0 None - 1 Pig 6.9 pKi = 6.9 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 909 10 7 11 2.3 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44419039 144174 0 None -1023 8 Human 6.9 pKi = 6.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1096 20 14 15 -4.6 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
CHEMBL375324 144174 0 None -1023 8 Human 6.9 pKi = 6.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1096 20 14 15 -4.6 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
46890187 14026 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 451 2 0 1 7.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2cc(Cl)c(-c3cccc4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1085851 14026 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 451 2 0 1 7.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2cc(Cl)c(-c3cccc4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
168272611 197165 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 574 8 1 5 6.2 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00567
CHEMBL5177490 197165 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 574 8 1 5 6.2 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00567
44314081 211746 0 None -2 2 Rat 5.9 pKi = 5.9 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 620 8 1 6 7.0 Cc1occc1C(=O)Nc1ccc(C(=O)N(C)c2ccccc2Oc2cccc(C(=O)N3CCC(N4CCCCC4)CC3)c2)cc1 10.1016/s0960-894x(01)00723-5
CHEMBL76498 211746 0 None -2 2 Rat 5.9 pKi = 5.9 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 620 8 1 6 7.0 Cc1occc1C(=O)Nc1ccc(C(=O)N(C)c2ccccc2Oc2cccc(C(=O)N3CCC(N4CCCCC4)CC3)c2)cc1 10.1016/s0960-894x(01)00723-5
44275104 104062 0 None -1737 4 Human 6.9 pKi = 6.9 Binding
Compound was tested for its ability to of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorCompound was tested for its ability to of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1127 32 14 14 -3.9 CN(C(=O)Cc1ccc(O)cc1)[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm9804782
CHEMBL269012 104062 0 None -1737 4 Human 6.9 pKi = 6.9 Binding
Compound was tested for its ability to of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorCompound was tested for its ability to of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1127 32 14 14 -3.9 CN(C(=O)Cc1ccc(O)cc1)[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm9804782
CHEMBL2369836 216480 0 None -2630 4 Human 5.9 pKi = 5.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
44520860 186399 0 None 4 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 548 5 1 6 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cnccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL474274 186399 0 None 4 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 548 5 1 6 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cnccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44520880 19349 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 550 5 1 4 6.0 CC1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2008.09.039
CHEMBL1186825 19349 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 550 5 1 4 6.0 CC1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2008.09.039
CHEMBL479918 19349 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 550 5 1 4 6.0 CC1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2008.09.039
44520882 19353 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 550 5 1 4 6.1 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1186831 19353 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 550 5 1 4 6.1 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL480104 19353 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 550 5 1 4 6.1 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
44520852 206487 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 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 10.1016/j.bmc.2009.10.038
CHEMBL593325 206487 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 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 10.1016/j.bmc.2009.10.038
44520851 206578 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 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 10.1016/j.bmc.2009.10.038
CHEMBL594026 206578 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 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 10.1016/j.bmc.2009.10.038
71453576 89155 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1357 31 4 17 9.0 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)[O-])cc3S(=O)(=O)NCCOCCOCCOCCn3cc(CNC(=O)CCC(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6-c6ccccc6)cc5)c5ccccc54)nn3)c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2172294 89155 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1357 31 4 17 9.0 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)[O-])cc3S(=O)(=O)NCCOCCOCCOCCn3cc(CNC(=O)CCC(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6-c6ccccc6)cc5)c5ccccc54)nn3)c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
71462477 89152 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1573 42 5 20 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
71482382 89152 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1573 42 5 20 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
CHEMBL2172291 89152 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1573 42 5 20 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
56665480 69982 0 None -91 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 754 6 2 8 3.5 CC[C@@H](C)[C@@H]1/N=C(\S)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
CHEMBL1790544 69982 0 None -91 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 754 6 2 8 3.5 CC[C@@H](C)[C@@H]1/N=C(\S)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
137637867 163000 0 None -50 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@@H](O)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL4064556 163000 0 None -50 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@@H](O)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.7b00422
70685417 80424 0 None -831 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation countingDisplacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 707 9 0 6 4.3 CS(=O)(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)CCc5ccccc54)CC3)c(OC/C=C/I)c2)CC1 10.1016/j.bmc.2012.02.019
CHEMBL2017867 80424 0 None -831 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation countingDisplacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 707 9 0 6 4.3 CS(=O)(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)CCc5ccccc54)CC3)c(OC/C=C/I)c2)CC1 10.1016/j.bmc.2012.02.019
10929819 113721 0 None -371 2 Human 4.8 pKi = 4.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 565 15 0 6 7.7 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCCCCCN1CCN(C)CC1 10.1021/jm010544r
CHEMBL314908 113721 0 None -371 2 Human 4.8 pKi = 4.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 565 15 0 6 7.7 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCCCCCN1CCN(C)CC1 10.1021/jm010544r
10208389 85406 0 None -10000 4 Human 4.8 pKi = 4.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 523 11 0 6 6.4 Cc1cccc(OCCCCCCN2CCN(C)CC2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
CHEMBL2112339 85406 0 None -10000 4 Human 4.8 pKi = 4.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 523 11 0 6 6.4 Cc1cccc(OCCCCCCN2CCN(C)CC2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
46890707 13499 0 None -19 2 Human 7.8 pKi = 7.8 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 419 3 0 3 6.6 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1csc2ccccc12 10.1016/j.bmcl.2010.04.068
CHEMBL1083703 13499 0 None -19 2 Human 7.8 pKi = 7.8 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 419 3 0 3 6.6 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1csc2ccccc12 10.1016/j.bmcl.2010.04.068
9807250 85122 0 None 58 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 O=C(Nc1ccc(C(=O)N2C[C@@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL2093899 85122 0 None 58 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 O=C(Nc1ccc(C(=O)N2C[C@@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL2110044 85122 0 None 58 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 O=C(Nc1ccc(C(=O)N2C[C@@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325733 214068 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 549 5 1 5 6.2 COc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CC2CSCCN2Cc2ccccc21 10.1016/j.bmcl.2004.03.083
CHEMBL93209 214068 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 549 5 1 5 6.2 COc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CC2CSCCN2Cc2ccccc21 10.1016/j.bmcl.2004.03.083
9938406 100092 1 None -213 6 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards rat kidney Vasopressin V2 receptor by using functional assayBinding affinity towards rat kidney Vasopressin V2 receptor by using functional assay
ChEMBL 589 7 0 6 4.7 CC(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)OCc5ccccc54)CC3)c(OCC(F)(F)F)c2)CC1 10.1016/s0960-894x(99)00181-x
CHEMBL24526 100092 1 None -213 6 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards rat kidney Vasopressin V2 receptor by using functional assayBinding affinity towards rat kidney Vasopressin V2 receptor by using functional assay
ChEMBL 589 7 0 6 4.7 CC(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)OCc5ccccc54)CC3)c(OCC(F)(F)F)c2)CC1 10.1016/s0960-894x(99)00181-x
CHEMBL1790548 215677 0 None -50 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 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]2CCCNN2C(=O)[C@H]2CCCNN2C1=O 10.1021/jm00171a003
CHEMBL1790548 215677 0 None -50 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 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]2CCCNN2C(=O)[C@H]2CCCNN2C1=O 10.1021/jm00171a003
2042 9757 58 None -831 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL None None None None 10.1021/jm501395b
2174 9757 58 None -831 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL None None None None 10.1021/jm501395b
2176 9757 58 None -831 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL None None None None 10.1021/jm501395b
439302 9757 58 None -831 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL None None None None 10.1021/jm501395b
CHEMBL395429 9757 58 None -831 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL None None None None 10.1021/jm501395b
DB00107 9757 58 None -831 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL None None None None 10.1021/jm501395b
54585227 67961 0 None -912 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1042 18 12 15 -1.9 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)C(O)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
CHEMBL1765669 67961 0 None -912 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1042 18 12 15 -1.9 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)C(O)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
44520856 195806 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 577 6 1 6 5.6 COc1cccc(CNC(=O)/C=C2/c3ccccc3N(C(=O)c3ccc(-n4ccc(C)n4)cc3Cl)CCC2(F)F)n1 10.1016/j.bmc.2009.03.001
CHEMBL509183 195806 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 577 6 1 6 5.6 COc1cccc(CNC(=O)/C=C2/c3ccccc3N(C(=O)c3ccc(-n4ccc(C)n4)cc3Cl)CCC2(F)F)n1 10.1016/j.bmc.2009.03.001
44520881 19350 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 550 5 1 4 6.1 CC1CCCN1c1ccc(C(=O)N2CCC(F)(F)/C(=C\C(=O)NCc3ccccn3)c3ccccc32)c(Cl)c1 10.1016/j.bmc.2008.09.039
CHEMBL1186826 19350 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 550 5 1 4 6.1 CC1CCCN1c1ccc(C(=O)N2CCC(F)(F)/C(=C\C(=O)NCc3ccccn3)c3ccccc32)c(Cl)c1 10.1016/j.bmc.2008.09.039
CHEMBL479919 19350 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 550 5 1 4 6.1 CC1CCCN1c1ccc(C(=O)N2CCC(F)(F)/C(=C\C(=O)NCc3ccccn3)c3ccccc32)c(Cl)c1 10.1016/j.bmc.2008.09.039
44520850 206643 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 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 10.1016/j.bmc.2009.10.038
CHEMBL594488 206643 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 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 10.1016/j.bmc.2009.10.038
71455306 89163 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1204 26 3 13 9.7 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NCCOCCOCCOCCC(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6-c6ccccc6)cc5)c5ccccc54)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2172393 89163 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1204 26 3 13 9.7 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NCCOCCOCCOCCC(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6-c6ccccc6)cc5)c5ccccc54)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
132822146 164019 0 None -23 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3c(C)cccc32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL4076436 164019 0 None -23 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3c(C)cccc32)cc1 10.1021/acs.jmedchem.7b00422
47177173 171221 1 None -3 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 377 1 0 1 4.3 O=C(c1ccc(I)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
CHEMBL4213812 171221 1 None -3 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 377 1 0 1 4.3 O=C(c1ccc(I)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
44335356 11997 0 None 5 2 Human 6.8 pKi = 6.8 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 385 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCNc3ccccc32)cc1 10.1016/s0960-894x(02)00649-2
CHEMBL106229 11997 0 None 5 2 Human 6.8 pKi = 6.8 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 385 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCNc3ccccc32)cc1 10.1016/s0960-894x(02)00649-2
CHEMBL1790542 215673 0 None -346 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 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]2CCC(=O)NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
CHEMBL339118 218396 0 None -19 2 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 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 10.1021/jm00169a001
44297525 103584 0 None -120226 3 Rat 4.8 pKi = 4.8 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1329 38 15 16 -1.8 CN(C(=O)CCc1cccc(N=[N+]=[N-])c1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
CHEMBL265048 103584 0 None -120226 3 Rat 4.8 pKi = 4.8 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1329 38 15 16 -1.8 CN(C(=O)CCc1cccc(N=[N+]=[N-])c1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
10444 9106 14 None -7 3 Human 5.8 pKi = 5.8 Binding
Displacement of DY647 from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells by TR-FRET assayDisplacement of DY647 from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
139030525 9106 14 None -7 3 Human 5.8 pKi = 5.8 Binding
Displacement of DY647 from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells by TR-FRET assayDisplacement of DY647 from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
145711714 9106 14 None -7 3 Human 5.8 pKi = 5.8 Binding
Displacement of DY647 from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells by TR-FRET assayDisplacement of DY647 from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
CHEMBL4204210 9106 14 None -7 3 Human 5.8 pKi = 5.8 Binding
Displacement of DY647 from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells by TR-FRET assayDisplacement of DY647 from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
53239961 73393 0 None -2 2 Rat 6.8 pKi = 6.8 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 491 2 3 5 5.1 Nc1nc(-c2ccc3c(c2)C(=Cc2cc(Br)c(O)c(Br)c2)C(=O)N3)cs1 10.1016/s0960-894x(01)00723-5
CHEMBL1794053 73393 0 None -2 2 Rat 6.8 pKi = 6.8 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 491 2 3 5 5.1 Nc1nc(-c2ccc3c(c2)C(=Cc2cc(Br)c(O)c(Br)c2)C(=O)N3)cs1 10.1016/s0960-894x(01)00723-5
CHEMBL1852697 73393 0 None -2 2 Rat 6.8 pKi = 6.8 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 491 2 3 5 5.1 Nc1nc(-c2ccc3c(c2)C(=Cc2cc(Br)c(O)c(Br)c2)C(=O)N3)cs1 10.1016/s0960-894x(01)00723-5
44325377 118365 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(-c2ccccc2)c(C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c1 10.1016/j.bmcl.2004.03.083
CHEMBL328227 118365 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(-c2ccccc2)c(C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c1 10.1016/j.bmcl.2004.03.083
132822145 166321 0 None -26 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL4102459 166321 0 None -26 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.7b00422
44520885 19222 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 565 5 1 5 4.9 CN1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)CC1 10.1016/j.bmc.2008.09.039
CHEMBL1186071 19222 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 565 5 1 5 4.9 CN1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)CC1 10.1016/j.bmc.2008.09.039
CHEMBL448269 19222 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 565 5 1 5 4.9 CN1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)CC1 10.1016/j.bmc.2008.09.039
46890154 13623 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 423 2 0 2 7.3 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3csc4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1084070 13623 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 423 2 0 2 7.3 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3csc4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
46890214 13868 0 None -1 2 Human 6.8 pKi = 6.8 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 417 2 0 1 7.2 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3cccc4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1085123 13868 0 None -1 2 Human 6.8 pKi = 6.8 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 417 2 0 1 7.2 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3cccc4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
2200 10084 46 None -177 6 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10.1021/jm010544r
3482 10084 46 None -177 6 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10.1021/jm010544r
60943 10084 46 None -177 6 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10.1021/jm010544r
CHEMBL419667 10084 46 None -177 6 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10.1021/jm010544r
DB13929 10084 46 None -177 6 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10.1021/jm010544r
10164478 213464 0 None -1698 4 Human 5.8 pKi = 5.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 509 11 0 6 6.1 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCN(C)CC1 10.1021/jm010544r
CHEMBL89552 213464 0 None -1698 4 Human 5.8 pKi = 5.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 509 11 0 6 6.1 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCN(C)CC1 10.1021/jm010544r
137648906 164161 0 None -22 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@@H](O)c3c(C)cccc32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL4078185 164161 0 None -22 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@@H](O)c3c(C)cccc32)cc1 10.1021/acs.jmedchem.7b00422
44520868 188807 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 498 5 1 4 5.4 CCCNC(=O)/C=C1/c2ccccc2N(C(=O)c2ccc(-n3ccc(C)n3)cc2Cl)CCC1(F)F 10.1016/j.bmc.2009.03.001
CHEMBL478083 188807 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 498 5 1 4 5.4 CCCNC(=O)/C=C1/c2ccccc2N(C(=O)c2ccc(-n3ccc(C)n3)cc2Cl)CCC1(F)F 10.1016/j.bmc.2009.03.001
44520874 19449 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 575 6 1 5 6.4 CC(C)c1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
CHEMBL1187362 19449 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 575 6 1 5 6.4 CC(C)c1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
CHEMBL500371 19449 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 575 6 1 5 6.4 CC(C)c1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
168277203 197418 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 588 8 1 5 6.5 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3CCCN(CCCN4CCOCC4)c4ccccc43)cc2)cc1 10.1021/acs.jmedchem.2c00567
CHEMBL5181318 197418 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 588 8 1 5 6.5 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3CCCN(CCCN4CCOCC4)c4ccccc43)cc2)cc1 10.1021/acs.jmedchem.2c00567
44325545 213907 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.5 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccc(F)c(F)c32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL92187 213907 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.5 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccc(F)c(F)c32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44335386 114787 0 None 14 2 Human 6.8 pKi = 6.8 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 489 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1F 10.1016/s0960-894x(02)00649-2
CHEMBL319433 114787 0 None 14 2 Human 6.8 pKi = 6.8 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 489 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1F 10.1016/s0960-894x(02)00649-2
57519948 80426 4 None -190 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to human V2R by competitive binding assayBinding affinity to human V2R by competitive binding assay
ChEMBL 587 9 0 6 3.4 CS(=O)(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)CCc5ccccc54)CC3)c(OCCF)c2)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL2017869 80426 4 None -190 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to human V2R by competitive binding assayBinding affinity to human V2R by competitive binding assay
ChEMBL 587 9 0 6 3.4 CS(=O)(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)CCc5ccccc54)CC3)c(OCCF)c2)CC1 10.1016/j.bmcl.2013.07.045
118734334 125375 0 None -10 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 416 3 1 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416767 125375 0 None -10 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 416 3 1 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
57519948 80426 4 None -190 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation countingDisplacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 587 9 0 6 3.4 CS(=O)(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)CCc5ccccc54)CC3)c(OCCF)c2)CC1 10.1016/j.bmc.2012.02.019
CHEMBL2017869 80426 4 None -190 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation countingDisplacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 587 9 0 6 3.4 CS(=O)(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)CCc5ccccc54)CC3)c(OCCF)c2)CC1 10.1016/j.bmc.2012.02.019
CHEMBL52176 222377 0 None -229 2 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 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 10.1021/jm00169a001
10483105 97455 1 None -34 4 Human 6.7 pKi = 6.7 Binding
Binding affinity to human V2 receptorBinding affinity to human V2 receptor
ChEMBL 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 10.1016/j.bmcl.2012.10.116
CHEMBL2391300 97455 1 None -34 4 Human 6.7 pKi = 6.7 Binding
Binding affinity to human V2 receptorBinding affinity to human V2 receptor
ChEMBL 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 10.1016/j.bmcl.2012.10.116
46890614 13445 0 None -416 2 Human 5.7 pKi = 5.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 397 3 0 2 6.1 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.068
CHEMBL1083443 13445 0 None -416 2 Human 5.7 pKi = 5.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 397 3 0 2 6.1 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.068
118734334 125375 0 None -10 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 416 3 1 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416767 125375 0 None -10 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 416 3 1 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
10304617 213006 0 None -1819 4 Rat 5.7 pKi = 5.7 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 625 8 0 6 7.9 Cc1cccc(OCc2ccc(C(=O)N3CCC(N4CCCCC4)CC3)cc2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
CHEMBL86667 213006 0 None -1819 4 Rat 5.7 pKi = 5.7 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 625 8 0 6 7.9 Cc1cccc(OCc2ccc(C(=O)N3CCC(N4CCCCC4)CC3)cc2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
71451750 89153 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1295 30 4 17 7.6 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)[O-])cc3S(=O)(=O)NCCOCCOCCOCCn3cc(CNC(=O)CCC(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6C)cc5)c5ccccc54)nn3)c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2172292 89153 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1295 30 4 17 7.6 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)[O-])cc3S(=O)(=O)NCCOCCOCCOCCn3cc(CNC(=O)CCC(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6C)cc5)c5ccccc54)nn3)c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
46890569 14069 0 None -74 2 Human 6.7 pKi = 6.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 439 4 0 2 7.1 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccccc1-c1ccccc1 10.1016/j.bmcl.2010.04.068
CHEMBL1086052 14069 0 None -74 2 Human 6.7 pKi = 6.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 439 4 0 2 7.1 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccccc1-c1ccccc1 10.1016/j.bmcl.2010.04.068
46890099 14073 0 None -331 2 Human 5.7 pKi = 5.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 414 3 0 3 6.0 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cnc2ccccc2c1 10.1016/j.bmcl.2010.04.068
CHEMBL1086068 14073 0 None -331 2 Human 5.7 pKi = 5.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 414 3 0 3 6.0 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cnc2ccccc2c1 10.1016/j.bmcl.2010.04.068
44520854 198712 0 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 546 5 1 4 6.2 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccc4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL520040 198712 0 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 546 5 1 4 6.2 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccc4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
9959174 201266 0 None -3 3 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from rat vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from rat vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
CHEMBL487164 201266 0 None -3 3 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from rat vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from rat vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
CHEMBL528996 201266 0 None -3 3 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from rat vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from rat vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
44294532 162543 0 None - 1 Pig 7.7 pKi = 7.7 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 910 15 8 11 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL405818 162543 0 None - 1 Pig 7.7 pKi = 7.7 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 910 15 8 11 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
10304617 213006 0 None -1905 4 Human 5.7 pKi = 5.7 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 625 8 0 6 7.9 Cc1cccc(OCc2ccc(C(=O)N3CCC(N4CCCCC4)CC3)cc2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
CHEMBL86667 213006 0 None -1905 4 Human 5.7 pKi = 5.7 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 625 8 0 6 7.9 Cc1cccc(OCc2ccc(C(=O)N3CCC(N4CCCCC4)CC3)cc2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
CHEMBL2369829 216475 0 None -1 4 Human 8.7 pKi = 8.7 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None CC[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](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
172997 9112 57 None 64 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2004.03.083
2238 9112 57 None 64 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2004.03.083
CHEMBL49429 9112 57 None 64 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2004.03.083
DB06666 9112 57 None 64 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2004.03.083
216237 10615 89 None 2 5 Human 8.6 pKi = 8.6 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00567
2226 10615 89 None 2 5 Human 8.6 pKi = 8.6 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00567
4110 10615 89 None 2 5 Human 8.6 pKi = 8.6 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00567
443894 10615 89 None 2 5 Human 8.6 pKi = 8.6 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00567
CHEMBL344159 10615 89 None 2 5 Human 8.6 pKi = 8.6 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00567
DB06212 10615 89 None 2 5 Human 8.6 pKi = 8.6 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00567
11740743 20880 0 None 1 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 384 3 1 2 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm3006146
CHEMBL119793 20880 0 None 1 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 384 3 1 2 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm3006146
44325345 118339 0 None 75 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 493 3 1 4 4.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2004.03.083
CHEMBL328079 118339 0 None 75 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 493 3 1 4 4.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2004.03.083
44325607 118933 0 None 660 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)cc1 10.1016/j.bmcl.2004.03.083
CHEMBL329026 118933 0 None 660 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)cc1 10.1016/j.bmcl.2004.03.083
44351500 124255 0 None -1 2 Pig 8.5 pKi = 8.5 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 995 16 10 12 0.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL339943 124255 0 None -1 2 Pig 8.5 pKi = 8.5 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 995 16 10 12 0.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44520853 192298 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccncc4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL486268 192298 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccncc4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44520878 19221 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 583 5 1 5 6.5 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3cc4ccccc4n3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1186070 19221 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 583 5 1 5 6.5 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3cc4ccccc4n3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL448195 19221 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 583 5 1 5 6.5 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3cc4ccccc4n3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
44563579 181370 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assayBinding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assay
ChEMBL 449 4 2 2 5.6 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL455699 181370 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assayBinding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assay
ChEMBL 449 4 2 2 5.6 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL5070075 221005 0 None -660 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL None None None O[C@@H]1Cc2cc(Cl)ccc2-n2c(nnc2[C@H]2CC[C@H](Oc3ccccn3)CC2)C1 10.1021/acs.jmedchem.1c00863
44520884 19224 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 579 6 1 5 5.3 CN(C)C1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2008.09.039
CHEMBL1186088 19224 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 579 6 1 5 5.3 CN(C)C1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2008.09.039
CHEMBL448942 19224 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 579 6 1 5 5.3 CN(C)C1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2008.09.039
2249 9008 18 None -54 6 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1021/jm901812z
9872389 9008 18 None -54 6 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1021/jm901812z
CHEMBL1253853 9008 18 None -54 6 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1021/jm901812z
10298385 197367 33 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assayBinding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL518043 197367 33 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assayBinding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
46890438 13358 0 None -4073 2 Human 6.7 pKi = 6.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 347 2 0 1 5.7 Cc1ccccc1-c1ccc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)cc1 10.1016/j.bmcl.2010.04.068
CHEMBL1083094 13358 0 None -4073 2 Human 6.7 pKi = 6.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 347 2 0 1 5.7 Cc1ccccc1-c1ccc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)cc1 10.1016/j.bmcl.2010.04.068
44314342 109863 0 None -6 2 Rat 5.7 pKi = 5.7 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 604 7 1 5 6.9 Cc1occc1C(=O)Nc1ccc(C(=O)N(C)c2ccccc2-c2ccc(C(=O)N3CCC(N4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(01)00723-5
CHEMBL307487 109863 0 None -6 2 Rat 5.7 pKi = 5.7 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 604 7 1 5 6.9 Cc1occc1C(=O)Nc1ccc(C(=O)N(C)c2ccccc2-c2ccc(C(=O)N3CCC(N4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(01)00723-5
46890054 13691 0 None -19 2 Human 5.7 pKi = 5.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 443 4 0 3 6.6 COc1ccc2cc(-c3ccc(C(=O)N4C[C@]5(C)C[C@H]4CC(C)(C)C5)cc3OC)ccc2c1 10.1016/j.bmcl.2010.04.068
CHEMBL1084386 13691 0 None -19 2 Human 5.7 pKi = 5.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 443 4 0 3 6.6 COc1ccc2cc(-c3ccc(C(=O)N4C[C@]5(C)C[C@H]4CC(C)(C)C5)cc3OC)ccc2c1 10.1016/j.bmcl.2010.04.068
46890185 13975 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 549 3 0 2 10.1 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3ccc(-c4csc5ccccc45)c4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1085624 13975 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 549 3 0 2 10.1 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3ccc(-c4csc5ccccc45)c4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
19608069 125374 0 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 402 3 1 3 5.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3ccccc32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416766 125374 0 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 402 3 1 3 5.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3ccccc32)cc1 10.1021/acs.jmedchem.5b00289
10119966 192167 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccnc4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL486064 192167 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccnc4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44520873 19469 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 561 6 1 5 5.9 CCc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
CHEMBL1187511 19469 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 561 6 1 5 5.9 CCc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
CHEMBL506111 19469 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 561 6 1 5 5.9 CCc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
16109440 168395 0 None -831 4 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 997 16 11 14 -2.3 CC(C)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](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL412973 168395 0 None -831 4 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 997 16 11 14 -2.3 CC(C)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](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
44520870 193732 0 None 10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 514 5 2 5 4.1 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCC(=O)O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL490249 193732 0 None 10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 514 5 2 5 4.1 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCC(=O)O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44520879 19506 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 536 5 1 4 5.7 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1187728 19506 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 536 5 1 4 5.7 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL516757 19506 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 536 5 1 4 5.7 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1790549 215678 0 None -18 2 Rat 5.7 pKi = 5.7 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL None None None CC[C@@H](C)[C@H]1C(=O)N2NCCC[C@@H]2C(=O)N2NCCC[C@H]2C(=O)N(C)[C@H](Cc2ccccc2)C(=O)N2CCC[C@H]2C(=O)N[C@H](Cc2ccccc2)C(=O)N1O 10.1021/jm00171a003
54584267 67959 0 None -35481 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1154 25 12 15 0.2 CC(C)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](CCCCNC(=O)CCCCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
CHEMBL1765667 67959 0 None -35481 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1154 25 12 15 0.2 CC(C)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](CCCCNC(=O)CCCCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
44314536 211779 0 None -1 2 Rat 5.7 pKi = 5.7 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 620 8 1 6 7.0 Cc1occc1C(=O)Nc1ccc(C(=O)N(C)c2ccccc2Oc2ccccc2C(=O)N2CCC(N3CCCCC3)CC2)cc1 10.1016/s0960-894x(01)00723-5
CHEMBL76763 211779 0 None -1 2 Rat 5.7 pKi = 5.7 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 620 8 1 6 7.0 Cc1occc1C(=O)Nc1ccc(C(=O)N(C)c2ccccc2Oc2ccccc2C(=O)N2CCC(N3CCCCC3)CC2)cc1 10.1016/s0960-894x(01)00723-5
168277882 197292 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 588 9 1 5 6.6 O=C(Nc1ccc(C(=O)N2CCCN(CCCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
CHEMBL5179440 197292 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 588 9 1 5 6.6 O=C(Nc1ccc(C(=O)N2CCCN(CCCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
2181 8113 42 None -14 7 Human 7.6 pKi = 7.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None None 10.1021/jm030611c
2182 8113 42 None -14 7 Human 7.6 pKi = 7.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None None 10.1021/jm030611c
27991 8113 42 None -14 7 Human 7.6 pKi = 7.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None None 10.1021/jm030611c
5311065 8113 42 None -14 7 Human 7.6 pKi = 7.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None None 10.1021/jm030611c
CHEMBL1429 8113 42 None -14 7 Human 7.6 pKi = 7.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None None 10.1021/jm030611c
CHEMBL264448 8113 42 None -14 7 Human 7.6 pKi = 7.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None None 10.1021/jm030611c
DB00035 8113 42 None -14 7 Human 7.6 pKi = 7.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None None 10.1021/jm030611c
46890153 13622 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 457 2 0 2 7.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2cc(Cl)c(-c3csc4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1084069 13622 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 457 2 0 2 7.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2cc(Cl)c(-c3csc4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
145975166 170572 0 None -3 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 328 2 0 2 4.7 O=C(c1ccc(-c2cccnc2)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
CHEMBL4205970 170572 0 None -3 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 328 2 0 2 4.7 O=C(c1ccc(-c2cccnc2)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
46890053 13628 0 None -141 2 Human 5.6 pKi = 5.6 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 413 3 0 2 6.6 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2010.04.068
CHEMBL1084112 13628 0 None -141 2 Human 5.6 pKi = 5.6 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 413 3 0 2 6.6 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2010.04.068
CHEMBL2369845 216487 0 None -30 4 Human 7.6 pKi = 7.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None CCC[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](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
CHEMBL2369838 216482 0 None -12 4 Human 7.6 pKi = 7.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
16109446 143383 0 None -630 4 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 983 15 11 14 -2.7 CC(C)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](CN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL373968 143383 0 None -630 4 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 983 15 11 14 -2.7 CC(C)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](CN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
44297632 108793 0 None -57 2 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 780 6 3 6 2.9 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)N2CCN(CC2)C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00169a001
CHEMBL301708 108793 0 None -57 2 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 780 6 3 6 2.9 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)N2CCN(CC2)C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00169a001
44316241 103964 0 None -1071 4 Human 6.6 pKi = 6.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1053 18 12 14 -2.6 CC(C)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](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm030611c
CHEMBL268306 103964 0 None -1071 4 Human 6.6 pKi = 6.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1053 18 12 14 -2.6 CC(C)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](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm030611c
5034737 213122 12 None -20 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 341 4 0 4 4.9 COc1ccccc1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
CHEMBL87351 213122 12 None -20 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 341 4 0 4 4.9 COc1ccccc1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
10142915 213199 0 None -549 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 523 12 0 6 6.5 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCCN1CCN(C)CC1 10.1021/jm010544r
CHEMBL87887 213199 0 None -549 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 523 12 0 6 6.5 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCCN1CCN(C)CC1 10.1021/jm010544r
46890055 13223 0 None -2290 2 Human 5.6 pKi = 5.6 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 398 3 0 3 5.5 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccnc1Cl 10.1016/j.bmcl.2010.04.068
CHEMBL1082493 13223 0 None -2290 2 Human 5.6 pKi = 5.6 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 398 3 0 3 5.5 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccnc1Cl 10.1016/j.bmcl.2010.04.068
42629368 189444 0 None 251 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 457 3 1 4 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL478902 189444 0 None 251 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 457 3 1 4 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44325895 214687 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2C[C@@H]3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL96731 214687 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2C[C@@H]3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
71460752 89160 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1001 14 2 9 10.1 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6-c6ccccc6)cc5)c5ccccc54)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2172390 89160 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1001 14 2 9 10.1 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6-c6ccccc6)cc5)c5ccccc54)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2372926 217093 0 None -5 2 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL None None None CCOc1ccc(C[C@H]2NC(=O)[C@@H]3CCCN3C(=O)[C@@H](Cc3ccccc3)N(C)C(=O)[C@@H]3CCCCN3C(=O)[C@H]3CCCCN3C(=O)[C@H]([C@@H](C)CC)NC2=O)cc1 10.1021/jm00169a001
1103817 23776 13 None -602 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]LVA antagonist from human vasopressin 2 receptor expressed in HEK293-EBNA cellsDisplacement of [125I]LVA antagonist from human vasopressin 2 receptor expressed in HEK293-EBNA cells
ChEMBL 492 8 2 6 3.1 CCOc1ccc(S(=O)(=O)N(CC(=O)N/N=C2\C(=O)Nc3ccccc32)c2ccc(C)cc2)cc1 10.1021/jm050645f
CHEMBL1254117 23776 13 None -602 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]LVA antagonist from human vasopressin 2 receptor expressed in HEK293-EBNA cellsDisplacement of [125I]LVA antagonist from human vasopressin 2 receptor expressed in HEK293-EBNA cells
ChEMBL 492 8 2 6 3.1 CCOc1ccc(S(=O)(=O)N(CC(=O)N/N=C2\C(=O)Nc3ccccc32)c2ccc(C)cc2)cc1 10.1021/jm050645f
1103817 23776 13 None -602 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 492 8 2 6 3.1 CCOc1ccc(S(=O)(=O)N(CC(=O)N/N=C2\C(=O)Nc3ccccc32)c2ccc(C)cc2)cc1 10.1021/jm901812z
CHEMBL1254117 23776 13 None -602 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 492 8 2 6 3.1 CCOc1ccc(S(=O)(=O)N(CC(=O)N/N=C2\C(=O)Nc3ccccc32)c2ccc(C)cc2)cc1 10.1021/jm901812z
42611262 187338 0 None -251 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]oxytocin from human vasopressin V2 receptor expressed in CHO cells by filtration binding assayDisplacement of [3H]oxytocin from human vasopressin V2 receptor expressed in CHO cells by filtration binding assay
ChEMBL 349 6 0 2 4.7 Cc1cc(C(=O)N(CC2CC2)CC2CCCO2)ccc1-c1ccccc1 10.1016/j.bmcl.2008.11.064
CHEMBL475395 187338 0 None -251 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]oxytocin from human vasopressin V2 receptor expressed in CHO cells by filtration binding assayDisplacement of [3H]oxytocin from human vasopressin V2 receptor expressed in CHO cells by filtration binding assay
ChEMBL 349 6 0 2 4.7 Cc1cc(C(=O)N(CC2CC2)CC2CCCO2)ccc1-c1ccccc1 10.1016/j.bmcl.2008.11.064
168270081 196833 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 560 7 1 5 5.8 O=C(Nc1ccc(C(=O)N2CCCN(CCN3CCOCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
CHEMBL5172250 196833 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 560 7 1 5 5.8 O=C(Nc1ccc(C(=O)N2CCCN(CCN3CCOCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
44294573 168878 0 None -3 2 Pig 7.6 pKi = 7.6 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 953 16 9 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL416114 168878 0 None -3 2 Pig 7.6 pKi = 7.6 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 953 16 9 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
71451749 89149 0 None 38 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1205 25 7 15 9.2 O=C(CCC(=O)NC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc21)NCc1cn(CCOCCOCCOCCNC(=S)Nc2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)nn1 10.1021/jm3006146
CHEMBL2172288 89149 0 None 38 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1205 25 7 15 9.2 O=C(CCC(=O)NC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc21)NCc1cn(CCOCCOCCOCCNC(=S)Nc2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)nn1 10.1021/jm3006146
CHEMBL300642 217687 0 None -32 2 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 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]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00169a001
44520866 188419 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 536 5 1 5 5.8 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccco4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL477456 188419 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 536 5 1 5 5.8 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccco4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44351385 123819 0 None - 1 Pig 7.6 pKi = 7.6 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 910 14 8 11 2.2 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)NCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL339073 123819 0 None - 1 Pig 7.6 pKi = 7.6 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 910 14 8 11 2.2 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)NCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44351440 175591 0 None - 1 Pig 7.6 pKi = 7.6 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 1036 17 8 12 3.0 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL437674 175591 0 None - 1 Pig 7.6 pKi = 7.6 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 1036 17 8 12 3.0 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44351357 162495 0 None - 1 Pig 7.6 pKi = 7.6 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 1055 14 8 12 3.1 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCc3ccc(CN)cc3)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL405308 162495 0 None - 1 Pig 7.6 pKi = 7.6 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 1055 14 8 12 3.1 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCc3ccc(CN)cc3)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
2253 9012 20 None -37153 6 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 586 7 0 7 4.4 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)Cc1ccc[n+](c1C)[O-] 10.1021/jm901812z
5311202 9012 20 None -37153 6 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 586 7 0 7 4.4 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)Cc1ccc[n+](c1C)[O-] 10.1021/jm901812z
CHEMBL306645 9012 20 None -37153 6 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 586 7 0 7 4.4 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)Cc1ccc[n+](c1C)[O-] 10.1021/jm901812z
145978570 170598 0 None -8 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 331 2 0 3 4.2 Cc1ccn(-c2ccc(C(=O)N3CCCCc4ccccc43)cc2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL4206233 170598 0 None -8 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 331 2 0 3 4.2 Cc1ccn(-c2ccc(C(=O)N3CCCCc4ccccc43)cc2)n1 10.1021/acs.jmedchem.8b00697
44275447 103198 0 None -354 4 Human 6.6 pKi = 6.6 Binding
The inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorThe inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1111 32 13 13 -3.6 CN(C(=O)Cc1ccccc1)[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm9804782
CHEMBL262035 103198 0 None -354 4 Human 6.6 pKi = 6.6 Binding
The inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorThe inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1111 32 13 13 -3.6 CN(C(=O)Cc1ccccc1)[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm9804782
2200 10084 46 None -288 6 Rat 6.5 pKi = 6.5 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10.1021/jm010544r
3482 10084 46 None -288 6 Rat 6.5 pKi = 6.5 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10.1021/jm010544r
60943 10084 46 None -288 6 Rat 6.5 pKi = 6.5 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10.1021/jm010544r
CHEMBL419667 10084 46 None -288 6 Rat 6.5 pKi = 6.5 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10.1021/jm010544r
DB13929 10084 46 None -288 6 Rat 6.5 pKi = 6.5 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10.1021/jm010544r
135916070 207752 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 418 2 1 6 4.5 Cc1ccn(-c2ccc(C(=O)N3Cc4cnn(C)c4Nc4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL601931 207752 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 418 2 1 6 4.5 Cc1ccn(-c2ccc(C(=O)N3Cc4cnn(C)c4Nc4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
135916070 207752 0 None -1 3 Human 7.5 pKi = 7.5 Binding
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
ChEMBL 418 2 1 6 4.5 Cc1ccn(-c2ccc(C(=O)N3Cc4cnn(C)c4Nc4ccccc43)c(Cl)c2)n1 10.1021/jm901084f
CHEMBL601931 207752 0 None -1 3 Human 7.5 pKi = 7.5 Binding
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
ChEMBL 418 2 1 6 4.5 Cc1ccn(-c2ccc(C(=O)N3Cc4cnn(C)c4Nc4ccccc43)c(Cl)c2)n1 10.1021/jm901084f
2202 9537 33 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation counting
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2011.03.012
9895468 9537 33 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation counting
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2011.03.012
CHEMBL582857 9537 33 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation counting
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2011.03.012
DB12643 9537 33 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation counting
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2011.03.012
9981665 125255 4 None -77 6 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue
ChEMBL 459 5 2 4 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CC(=O)O)C2 10.1021/jm901812z
CHEMBL341339 125255 4 None -77 6 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue
ChEMBL 459 5 2 4 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CC(=O)O)C2 10.1021/jm901812z
46890615 13446 0 None -128 2 Human 6.5 pKi = 6.5 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 411 3 0 2 6.4 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccc(Cl)cc1C 10.1016/j.bmcl.2010.04.068
CHEMBL1083444 13446 0 None -128 2 Human 6.5 pKi = 6.5 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 411 3 0 2 6.4 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccc(Cl)cc1C 10.1016/j.bmcl.2010.04.068
44297517 162505 0 None -28 3 Rat 8.5 pKi = 8.5 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1343 39 15 16 -1.4 CN(C(=O)CCCc1ccc(N=[N+]=[N-])cc1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
CHEMBL405440 162505 0 None -28 3 Rat 8.5 pKi = 8.5 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1343 39 15 16 -1.4 CN(C(=O)CCCc1ccc(N=[N+]=[N-])cc1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
151171 7947 50 None -2 6 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1021/acs.jmedchem.8b00697
216322 7947 50 None -2 6 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1021/acs.jmedchem.8b00697
2203 7947 50 None -2 6 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1021/acs.jmedchem.8b00697
732 7947 50 None -2 6 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1021/acs.jmedchem.8b00697
CHEMBL1755 7947 50 None -2 6 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1021/acs.jmedchem.8b00697
DB00872 7947 50 None -2 6 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1021/acs.jmedchem.8b00697
44419029 103685 0 None -77 4 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1053 18 13 14 -2.4 CC(C)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 10.1021/jm060928n
CHEMBL265859 103685 0 None -77 4 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1053 18 13 14 -2.4 CC(C)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 10.1021/jm060928n
16109448 148378 0 None -5 4 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1054 19 14 15 -3.7 N=C(N)NCCC[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](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL385068 148378 0 None -5 4 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1054 19 14 15 -3.7 N=C(N)NCCC[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](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
44325579 118704 0 None 33 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 535 4 2 5 5.9 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(O)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL328791 118704 0 None 33 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 535 4 2 5 5.9 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(O)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
10414302 119297 0 None 50 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2C[C@H]3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL329903 119297 0 None 50 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2C[C@H]3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44294573 168878 0 None 3 2 Human 8.5 pKi = 8.5 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidney
ChEMBL 953 16 9 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL416114 168878 0 None 3 2 Human 8.5 pKi = 8.5 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidney
ChEMBL 953 16 9 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
11366713 144000 0 None -7 8 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1054 19 13 15 -3.9 NCCC[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](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL375096 144000 0 None -7 8 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1054 19 13 15 -3.9 NCCC[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](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
44520861 187598 0 None 12 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 548 5 1 6 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccnn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL475684 187598 0 None 12 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 548 5 1 6 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccnn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL2370646 216684 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidney
ChEMBL None None None CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44351441 103653 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidney
ChEMBL 1050 16 9 12 1.5 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCN=C(N)N)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL265591 103653 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidney
ChEMBL 1050 16 9 12 1.5 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCN=C(N)N)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44325691 19770 0 None 239 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 1 4 6.8 O=C(Nc1ccc(C(=O)N2C[C@H]3CSCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL1189693 19770 0 None 239 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 1 4 6.8 O=C(Nc1ccc(C(=O)N2C[C@H]3CSCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL539285 19770 0 None 239 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 1 4 6.8 O=C(Nc1ccc(C(=O)N2C[C@H]3CSCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325766 119336 0 None 109 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 571 4 1 4 7.0 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1)c1ccc(F)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL330005 119336 0 None 109 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 571 4 1 4 7.0 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1)c1ccc(F)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325695 174785 0 None 1230 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1cccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c1 10.1016/j.bmcl.2004.03.083
CHEMBL432043 174785 0 None 1230 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1cccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c1 10.1016/j.bmcl.2004.03.083
44325332 214170 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 503 4 1 4 5.5 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL93861 214170 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 503 4 1 4 5.5 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
16109442 144175 0 None -6 4 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1068 20 14 15 -3.3 N=C(N)NCCC[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](CCCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL375325 144175 0 None -6 4 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1068 20 14 15 -3.3 N=C(N)NCCC[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](CCCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
163408867 199141 4 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 588 7 2 5 5.5 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCC(=O)N3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5207224 199141 4 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 588 7 2 5 5.5 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCC(=O)N3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
44294542 103258 0 None - 1 Pig 8.4 pKi = 8.4 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00162a001
CHEMBL262423 103258 0 None - 1 Pig 8.4 pKi = 8.4 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00162a001
44294542 103258 0 None - 1 Pig 8.4 pKi = 8.4 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL262423 103258 0 None - 1 Pig 8.4 pKi = 8.4 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
46890612 13676 0 None -81 2 Human 7.5 pKi = 7.5 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 420 4 1 3 5.4 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc(NC(C)=O)c1 10.1016/j.bmcl.2010.04.068
CHEMBL1084325 13676 0 None -81 2 Human 7.5 pKi = 7.5 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 420 4 1 3 5.4 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc(NC(C)=O)c1 10.1016/j.bmcl.2010.04.068
11757222 114779 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 547 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2C[C@H]3C4CCC(C4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
CHEMBL319418 114779 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 547 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2C[C@H]3C4CCC(C4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
44294592 103533 0 None - 1 Pig 7.5 pKi = 7.5 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1007 16 8 12 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@@H]3C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL264540 103533 0 None - 1 Pig 7.5 pKi = 7.5 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1007 16 8 12 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@@H]3C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
56679085 69983 0 None - 1 Rat 4.5 pKi = 4.5 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 724 6 2 8 2.7 CC[C@@H](C)[C@@H]1NC[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
CHEMBL1790550 69983 0 None - 1 Rat 4.5 pKi = 4.5 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 724 6 2 8 2.7 CC[C@@H](C)[C@@H]1NC[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
167184706 196764 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 588 9 2 5 6.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5171014 196764 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 588 9 2 5 6.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
167184778 196830 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 560 10 2 4 7.0 CCN(CC)CCCNC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2C)c2ccc(Cl)cc21 10.1021/acs.jmedchem.2c00011
CHEMBL5172177 196830 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 560 10 2 4 7.0 CCN(CC)CCCNC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2C)c2ccc(Cl)cc21 10.1021/acs.jmedchem.2c00011
53349471 125381 0 None -22 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 413 3 1 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(C)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416774 125381 0 None -22 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 413 3 1 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(C)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL1790552 215680 0 None -1 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 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]2CCCN(C)N2C(=O)[C@H]2CCCN(C)N2C1=O 10.1021/jm00171a003
54582318 67960 0 None -8317 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1210 29 12 15 1.7 CC(C)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](CCCCNC(=O)CCCCCCCCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
CHEMBL1765668 67960 0 None -8317 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1210 29 12 15 1.7 CC(C)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](CCCCNC(=O)CCCCCCCCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
11465834 145200 0 None -263 4 Human 6.5 pKi = 6.5 Binding
Displacement of vasopressin from human V2RDisplacement of vasopressin from human V2R
ChEMBL 483 6 1 3 3.3 CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)N(C)C)c1ccc(F)cc1F 10.1021/jm060073e
CHEMBL377414 145200 0 None -263 4 Human 6.5 pKi = 6.5 Binding
Displacement of vasopressin from human V2RDisplacement of vasopressin from human V2R
ChEMBL 483 6 1 3 3.3 CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)N(C)C)c1ccc(F)cc1F 10.1021/jm060073e
2168 10748 38 None -15 9 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting methodDisplacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2018.03.019
2810 10748 38 None -15 9 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting methodDisplacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2018.03.019
644077 10748 38 None -15 9 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting methodDisplacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2018.03.019
CHEMBL373742 10748 38 None -15 9 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting methodDisplacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2018.03.019
DB00067 10748 38 None -15 9 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting methodDisplacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2018.03.019
44335345 11943 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 505 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(02)00649-2
CHEMBL105961 11943 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 505 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(02)00649-2
CHEMBL2372927 217094 0 None -199 2 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]2CCCCN2C(=O)[C@@H]2CCCCN2C1=O 10.1021/jm00169a001
2202 9537 33 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptorDisplacement of [3H]AVP from human vasopressin V2 receptor
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2010.12.081
9895468 9537 33 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptorDisplacement of [3H]AVP from human vasopressin V2 receptor
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2010.12.081
CHEMBL582857 9537 33 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptorDisplacement of [3H]AVP from human vasopressin V2 receptor
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2010.12.081
DB12643 9537 33 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptorDisplacement of [3H]AVP from human vasopressin V2 receptor
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2010.12.081
2202 9537 33 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Arg8-vasopressin from human vasopressin V2 receptor expressed in CHO-K1 cells by Packard Topcount scintillation counterDisplacement of [3H]Arg8-vasopressin from human vasopressin V2 receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2009.09.050
9895468 9537 33 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Arg8-vasopressin from human vasopressin V2 receptor expressed in CHO-K1 cells by Packard Topcount scintillation counterDisplacement of [3H]Arg8-vasopressin from human vasopressin V2 receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2009.09.050
CHEMBL582857 9537 33 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Arg8-vasopressin from human vasopressin V2 receptor expressed in CHO-K1 cells by Packard Topcount scintillation counterDisplacement of [3H]Arg8-vasopressin from human vasopressin V2 receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2009.09.050
DB12643 9537 33 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Arg8-vasopressin from human vasopressin V2 receptor expressed in CHO-K1 cells by Packard Topcount scintillation counterDisplacement of [3H]Arg8-vasopressin from human vasopressin V2 receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2009.09.050
44520867 188805 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 456 3 1 4 4.4 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(N)=O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL478082 188805 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 456 3 1 4 4.4 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(N)=O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44314134 111569 0 None -331 2 Rat 7.5 pKi = 7.5 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 576 5 1 5 5.5 Cc1occc1C(=O)Nc1ccc(C(=O)N2CCC(F)(F)/C(=C/C(=O)N3CCC(N(C)C)CC3)c3ccccc32)cc1 10.1016/s0960-894x(01)00723-5
CHEMBL310921 111569 0 None -331 2 Rat 7.5 pKi = 7.5 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 576 5 1 5 5.5 Cc1occc1C(=O)Nc1ccc(C(=O)N2CCC(F)(F)/C(=C/C(=O)N3CCC(N(C)C)CC3)c3ccccc32)cc1 10.1016/s0960-894x(01)00723-5
2213 7306 46 None -660 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL None None None None 10.1016/j.bmcl.2007.11.008
3008 7306 46 None -660 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL None None None None 10.1016/j.bmcl.2007.11.008
5311010 7306 46 None -660 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL None None None None 10.1016/j.bmcl.2007.11.008
68613 7306 46 None -660 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL None None None None 10.1016/j.bmcl.2007.11.008
CHEMBL378642 7306 46 None -660 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL None None None None 10.1016/j.bmcl.2007.11.008
CHEMBL382301 7306 46 None -660 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL None None None None 10.1016/j.bmcl.2007.11.008
DB09059 7306 46 None -660 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL None None None None 10.1016/j.bmcl.2007.11.008
CHEMBL52813 222484 0 None -23 2 Rat 4.5 pKi = 4.5 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 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]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/jm00169a001
145966126 170923 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 408 3 0 4 4.9 Cc1ccn(-c2ccc(C(=O)N3CCCC(N(C)C)c4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL4210158 170923 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 408 3 0 4 4.9 Cc1ccn(-c2ccc(C(=O)N3CCCC(N(C)C)c4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
145964296 170905 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 329 2 0 3 4.1 O=C(c1ccc(-c2ncccn2)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
CHEMBL4209952 170905 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 329 2 0 3 4.1 O=C(c1ccc(-c2ncccn2)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
46890439 13359 1 None -51 2 Human 5.5 pKi = 5.5 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 347 2 0 1 5.7 Cc1ccccc1-c1ccc(C(=O)N2C[C@@]3(C)C[C@@H]2CC(C)(C)C3)cc1 10.1016/j.bmcl.2010.04.068
CHEMBL1083095 13359 1 None -51 2 Human 5.5 pKi = 5.5 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 347 2 0 1 5.7 Cc1ccccc1-c1ccc(C(=O)N2C[C@@]3(C)C[C@@H]2CC(C)(C)C3)cc1 10.1016/j.bmcl.2010.04.068
CHEMBL1790549 215678 0 None -18 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL None None None CC[C@@H](C)[C@H]1C(=O)N2NCCC[C@@H]2C(=O)N2NCCC[C@H]2C(=O)N(C)[C@H](Cc2ccccc2)C(=O)N2CCC[C@H]2C(=O)N[C@H](Cc2ccccc2)C(=O)N1O 10.1021/jm00171a003
45103785 206045 0 None -1 2 Human 5.5 pKi = 5.5 Binding
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
ChEMBL 584 4 1 5 4.6 Cc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1021/jm901084f
CHEMBL590175 206045 0 None -1 2 Human 5.5 pKi = 5.5 Binding
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
ChEMBL 584 4 1 5 4.6 Cc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1021/jm901084f
168281863 197819 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 608 8 1 5 6.8 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccc(Cl)cc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
CHEMBL5187046 197819 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 608 8 1 5 6.8 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccc(Cl)cc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
2042 9757 58 None -831 8 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL None None None None 10.1021/jm010526+
2174 9757 58 None -831 8 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL None None None None 10.1021/jm010526+
2176 9757 58 None -831 8 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL None None None None 10.1021/jm010526+
439302 9757 58 None -831 8 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL None None None None 10.1021/jm010526+
CHEMBL395429 9757 58 None -831 8 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL None None None None 10.1021/jm010526+
DB00107 9757 58 None -831 8 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL None None None None 10.1021/jm010526+
44361522 128473 0 None -6165 5 Rat 4.5 pKi = 4.5 Binding
Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from ratsBinding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats
ChEMBL 477 4 0 5 3.8 CC(=O)N1CCC(Oc2ccc(C(=O)N3CCC(N4C(=O)OCc5ccccc54)CC3)cc2)CC1 10.1021/jm00023a002
CHEMBL358793 128473 0 None -6165 5 Rat 4.5 pKi = 4.5 Binding
Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from ratsBinding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats
ChEMBL 477 4 0 5 3.8 CC(=O)N1CCC(Oc2ccc(C(=O)N3CCC(N4C(=O)OCc5ccccc54)CC3)cc2)CC1 10.1021/jm00023a002
44361406 41788 0 None -1122 5 Rat 4.5 pKi = 4.5 Binding
Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats.Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats.
ChEMBL 451 7 1 5 3.4 CC(=O)NCCCOc1ccc(C(=O)N2CCC(N3C(=O)OCc4ccccc43)CC2)cc1 10.1021/jm00023a002
CHEMBL143304 41788 0 None -1122 5 Rat 4.5 pKi = 4.5 Binding
Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats.Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats.
ChEMBL 451 7 1 5 3.4 CC(=O)NCCCOc1ccc(C(=O)N2CCC(N3C(=O)OCc4ccccc43)CC2)cc1 10.1021/jm00023a002
46890184 13307 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 453 3 0 3 7.3 COc1cc(-c2csc3ccccc23)c(Cl)cc1C(=O)N1C[C@]2(C)C[C@H]1CC(C)(C)C2 10.1016/j.bmcl.2010.04.068
CHEMBL1082835 13307 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 453 3 0 3 7.3 COc1cc(-c2csc3ccccc23)c(Cl)cc1C(=O)N1C[C@]2(C)C[C@H]1CC(C)(C)C2 10.1016/j.bmcl.2010.04.068
CHEMBL2369841 216485 0 None -10 4 Human 7.4 pKi = 7.4 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None NC[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](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
118734334 125375 0 None -10 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 416 3 1 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416767 125375 0 None -10 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 416 3 1 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
10187283 212992 0 None -120 4 Rat 6.4 pKi = 6.4 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 543 7 0 6 5.9 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCc1ccc(C(=O)N2CCN(C)CC2)cc1 10.1021/jm010544r
CHEMBL86577 212992 0 None -120 4 Rat 6.4 pKi = 6.4 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 543 7 0 6 5.9 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCc1ccc(C(=O)N2CCN(C)CC2)cc1 10.1021/jm010544r
44325905 171056 0 None 275 2 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 571 4 1 4 7.0 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1)c1cc(F)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL421180 171056 0 None 275 2 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 571 4 1 4 7.0 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1)c1cc(F)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44294507 103269 0 None - 1 Pig 7.4 pKi = 7.4 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1051 17 9 13 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL262499 103269 0 None - 1 Pig 7.4 pKi = 7.4 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1051 17 9 13 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL54443 222497 0 None -70 2 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 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]2CCNCN2C1=O 10.1021/jm00169a001
57520031 80431 0 None -131 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation countingDisplacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 555 7 0 6 3.0 COc1cc(OC2CCN(S(C)(=O)=O)CC2)ccc1CC(=O)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmc.2012.02.019
CHEMBL2017979 80431 0 None -131 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation countingDisplacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 555 7 0 6 3.0 COc1cc(OC2CCN(S(C)(=O)=O)CC2)ccc1CC(=O)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmc.2012.02.019
2252 9011 48 None -10000 5 Human 4.4 pKi = 4.4 Binding
Binding affinity towards human kidney Vasopressin V2 receptor by using functional assayBinding affinity towards human kidney Vasopressin V2 receptor by using functional assay
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1016/s0960-894x(99)00181-x
6918320 9011 48 None -10000 5 Human 4.4 pKi = 4.4 Binding
Binding affinity towards human kidney Vasopressin V2 receptor by using functional assayBinding affinity towards human kidney Vasopressin V2 receptor by using functional assay
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1016/s0960-894x(99)00181-x
CHEMBL24781 9011 48 None -10000 5 Human 4.4 pKi = 4.4 Binding
Binding affinity towards human kidney Vasopressin V2 receptor by using functional assayBinding affinity towards human kidney Vasopressin V2 receptor by using functional assay
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1016/s0960-894x(99)00181-x
2252 9011 48 None -10000 5 Human 4.4 pKi = 4.4 Binding
Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from early postmortem human donorsBinding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from early postmortem human donors
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1021/jm00023a002
6918320 9011 48 None -10000 5 Human 4.4 pKi = 4.4 Binding
Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from early postmortem human donorsBinding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from early postmortem human donors
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1021/jm00023a002
CHEMBL24781 9011 48 None -10000 5 Human 4.4 pKi = 4.4 Binding
Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from early postmortem human donorsBinding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from early postmortem human donors
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1021/jm00023a002
2252 9011 48 None -10000 5 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1021/jm901812z
6918320 9011 48 None -10000 5 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1021/jm901812z
CHEMBL24781 9011 48 None -10000 5 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1021/jm901812z
145976595 170494 0 None 6 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 408 2 1 4 4.9 Cc1ccn(C(=O)Nc2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL4205046 170494 0 None 6 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 408 2 1 4 4.9 Cc1ccn(C(=O)Nc2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
2204 10889 5 None -1258 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranesDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes
ChEMBL 616 5 1 5 6.4 O=C(N1CCC(CC1)N1CCCCC1)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccoc1C 10.1021/acs.jmedchem.8b00697
9917025 10889 5 None -1258 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranesDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes
ChEMBL 616 5 1 5 6.4 O=C(N1CCC(CC1)N1CCCCC1)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccoc1C 10.1021/acs.jmedchem.8b00697
CHEMBL3307200 10889 5 None -1258 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranesDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes
ChEMBL 616 5 1 5 6.4 O=C(N1CCC(CC1)N1CCCCC1)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccoc1C 10.1021/acs.jmedchem.8b00697
168282087 197536 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 602 10 2 5 6.8 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5182998 197536 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 602 10 2 5 6.8 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
46890215 13925 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 447 3 0 2 7.2 COc1cc(-c2cccc3ccccc23)c(Cl)cc1C(=O)N1C[C@]2(C)C[C@H]1CC(C)(C)C2 10.1016/j.bmcl.2010.04.068
CHEMBL1085378 13925 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 447 3 0 2 7.2 COc1cc(-c2cccc3ccccc23)c(Cl)cc1C(=O)N1C[C@]2(C)C[C@H]1CC(C)(C)C2 10.1016/j.bmcl.2010.04.068
11465834 145200 0 None -263 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 483 6 1 3 3.3 CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)N(C)C)c1ccc(F)cc1F 10.1021/jm201287w
CHEMBL377414 145200 0 None -263 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 483 6 1 3 3.3 CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)N(C)C)c1ccc(F)cc1F 10.1021/jm201287w
3537 10776 22 None 3 3 Human 7.4 pKi = 7.4 Binding
Binding affinity to V2 receptor (unknown origin)Binding affinity to V2 receptor (unknown origin)
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/acs.jmedchem.8b00697
5311500 10776 22 None 3 3 Human 7.4 pKi = 7.4 Binding
Binding affinity to V2 receptor (unknown origin)Binding affinity to V2 receptor (unknown origin)
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/acs.jmedchem.8b00697
CHEMBL363910 10776 22 None 3 3 Human 7.4 pKi = 7.4 Binding
Binding affinity to V2 receptor (unknown origin)Binding affinity to V2 receptor (unknown origin)
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/acs.jmedchem.8b00697
CHEMBL1790547 215676 0 None -57 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 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]2C=CC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
CHEMBL1790543 215674 0 None -61 2 Rat 5.4 pKi = 5.4 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 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]2CCC(=O)NN2C(=O)[C@H]2CCCNN2C1=O 10.1021/jm00171a003
11634973 82114 15 None -31622 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 518 6 1 5 2.8 CC[C@H](C)[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)N1CCOCC1)c1ccc(C)nc1C 10.1021/jm201287w
CHEMBL2037511 82114 15 None -31622 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 518 6 1 5 2.8 CC[C@H](C)[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)N1CCOCC1)c1ccc(C)nc1C 10.1021/jm201287w
71462479 89156 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1357 31 4 17 9.0 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NCCOCCOCCOCCn4cc(CNC(=O)CCC(=O)NC5CCCN(C(=O)c6ccc(NC(=O)c7ccccc7-c7ccccc7)cc6)c6ccccc65)nn4)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2172295 89156 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1357 31 4 17 9.0 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NCCOCCOCCOCCn4cc(CNC(=O)CCC(=O)NC5CCCN(C(=O)c6ccc(NC(=O)c7ccccc7-c7ccccc7)cc6)c6ccccc65)nn4)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2370640 216682 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidney
ChEMBL None None None CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44325363 113387 0 None 281 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c(-c2ccccc2)c1 10.1016/j.bmcl.2004.03.083
CHEMBL314290 113387 0 None 281 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c(-c2ccccc2)c1 10.1016/j.bmcl.2004.03.083
44325538 119338 0 None 616 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccc(O)cc1 10.1016/j.bmcl.2004.03.083
CHEMBL330016 119338 0 None 616 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccc(O)cc1 10.1016/j.bmcl.2004.03.083
168294659 199180 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 574 8 1 5 6.2 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
CHEMBL5207885 199180 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 574 8 1 5 6.2 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
CHEMBL2370646 216684 0 None -1 2 Pig 8.4 pKi = 8.4 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL None None None CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL408474 219494 0 None - 1 Pig 8.3 pKi = 8.3 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL None None None NCCCC[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(=O)O 10.1021/jm00150a003
73348509 96195 0 None 1 2 Pig 8.3 pKi = 8.3 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 979 13 8 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)NCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL2370642 96195 0 None 1 2 Pig 8.3 pKi = 8.3 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 979 13 8 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)NCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
9959174 201266 0 None 3 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL487164 201266 0 None 3 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL528996 201266 0 None 3 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
9959174 201266 0 None 3 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
CHEMBL487164 201266 0 None 3 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
CHEMBL528996 201266 0 None 3 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
73348509 96195 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidney
ChEMBL 979 13 8 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)NCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL2370642 96195 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidney
ChEMBL 979 13 8 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)NCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
15416417 166522 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 400 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@H](O)c3ccccc32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL4104877 166522 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 400 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@H](O)c3ccccc32)cc1 10.1021/acs.jmedchem.7b00422
44382498 103268 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1093 17 10 13 0.6 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCC(C)CC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
CHEMBL262482 103268 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1093 17 10 13 0.6 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCC(C)CC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
46890288 14197 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 528 3 0 2 8.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3ccc(-c4cccc5cccnc45)cc3Cl)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1086574 14197 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 528 3 0 2 8.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3ccc(-c4cccc5cccnc45)cc3Cl)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
44314382 109771 0 None -14 2 Rat 7.4 pKi = 7.4 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 648 9 1 6 7.1 Cc1ccc(N(C)C(=O)c2ccc(NC(=O)c3ccoc3C)cc2)c(OCc2ccc(C(=O)N3CCC(N4CCCCC4)CC3)cc2)c1 10.1016/s0960-894x(01)00723-5
CHEMBL306718 109771 0 None -14 2 Rat 7.4 pKi = 7.4 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 648 9 1 6 7.1 Cc1ccc(N(C)C(=O)c2ccc(NC(=O)c3ccoc3C)cc2)c(OCc2ccc(C(=O)N3CCC(N4CCCCC4)CC3)cc2)c1 10.1016/s0960-894x(01)00723-5
44351409 103396 0 None - 1 Pig 7.4 pKi = 7.4 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 1050 18 8 12 3.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL263432 103396 0 None - 1 Pig 7.4 pKi = 7.4 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 1050 18 8 12 3.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
46890290 13769 0 None -58 2 Human 6.4 pKi = 6.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 544 3 0 2 9.4 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3ccc(-c4cccc5cccnc45)c4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1084717 13769 0 None -58 2 Human 6.4 pKi = 6.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 544 3 0 2 9.4 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3ccc(-c4cccc5cccnc45)c4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
16109445 144022 0 None -1659 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1011 17 11 14 -1.9 CC(C)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](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL375188 144022 0 None -1659 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1011 17 11 14 -1.9 CC(C)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](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
46890289 14198 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 558 4 0 3 8.9 COc1cc(-c2cccc3cccnc23)c(Cl)cc1-c1ccc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)c(Cl)c1 10.1016/j.bmcl.2010.04.068
CHEMBL1086575 14198 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 558 4 0 3 8.9 COc1cc(-c2cccc3cccnc23)c(Cl)cc1-c1ccc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)c(Cl)c1 10.1016/j.bmcl.2010.04.068
CHEMBL2369848 216489 0 None -912 4 Human 5.4 pKi = 5.4 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
11016093 174834 0 None -2089 2 Human 5.4 pKi = 5.4 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 466 9 1 5 6.5 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCC1CCNCC1 10.1021/jm010544r
CHEMBL432375 174834 0 None -2089 2 Human 5.4 pKi = 5.4 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 466 9 1 5 6.5 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCC1CCNCC1 10.1021/jm010544r
44313913 211619 0 None -58 2 Rat 6.4 pKi = 6.4 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 670 10 1 7 6.2 CCc1nccn1-c1ccccc1C(=O)Nc1ccc(C(=O)N(C)c2ccc(C)cc2OCc2ccc(C(=O)N3CCN(C)CC3)cc2)cc1 10.1016/s0960-894x(01)00723-5
CHEMBL75489 211619 0 None -58 2 Rat 6.4 pKi = 6.4 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 670 10 1 7 6.2 CCc1nccn1-c1ccccc1C(=O)Nc1ccc(C(=O)N(C)c2ccc(C)cc2OCc2ccc(C(=O)N3CCN(C)CC3)cc2)cc1 10.1016/s0960-894x(01)00723-5
16109438 103352 0 None -147 5 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1051 17 11 14 -1.0 NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
CHEMBL263090 103352 0 None -147 5 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1051 17 11 14 -1.0 NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
16109444 168228 0 None -562 5 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1037 16 11 14 -1.3 NCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
CHEMBL412742 168228 0 None -562 5 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1037 16 11 14 -1.3 NCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
CHEMBL297725 217681 0 None -31 2 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 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 10.1021/jm00169a001
54584268 67962 0 None -5370 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1226 29 13 16 0.7 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)C(O)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCNC(=O)CCCCCCCCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
CHEMBL1765671 67962 0 None -5370 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1226 29 13 16 0.7 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)C(O)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCNC(=O)CCCCCCCCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
137652605 165613 0 None -22 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@H](O)c3c(C)cccc32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL4094707 165613 0 None -22 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@H](O)c3c(C)cccc32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL2371439 216824 0 None - 1 Pig 7.3 pKi = 7.3 Binding
Inhibition of LVP-sensitive adenylate cyclase in a pig renal medullary preparationInhibition of LVP-sensitive adenylate cyclase in a pig renal medullary preparation
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CC(C2CCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00399a009
26434734 170296 8 None -5 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 294 2 0 2 3.7 CN(C)c1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/acs.jmedchem.8b00697
CHEMBL4202525 170296 8 None -5 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 294 2 0 2 3.7 CN(C)c1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/acs.jmedchem.8b00697
CHEMBL5070261 221008 0 None -1548 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL None None None OC1Cc2cc(Cl)ccc2-n2c(nnc2[C@H]2CC[C@H](Oc3ccccn3)CC2)C1 10.1021/acs.jmedchem.1c00863
53349364 173468 0 None -8 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHO cell membranes after 60 minsDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHO cell membranes after 60 mins
ChEMBL 427 3 1 3 4.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC(=O)N(C)c3cccc(C)c32)cc1 10.1039/C8MD00033F
CHEMBL4282161 173468 0 None -8 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHO cell membranes after 60 minsDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHO cell membranes after 60 mins
ChEMBL 427 3 1 3 4.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC(=O)N(C)c3cccc(C)c32)cc1 10.1039/C8MD00033F
46890485 13802 0 None -7943 2 Human 6.3 pKi = 6.3 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 361 2 0 1 6.0 Cc1ccccc1-c1ccc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)cc1C 10.1016/j.bmcl.2010.04.068
CHEMBL1084823 13802 0 None -7943 2 Human 6.3 pKi = 6.3 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 361 2 0 1 6.0 Cc1ccccc1-c1ccc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)cc1C 10.1016/j.bmcl.2010.04.068
CHEMBL300103 217686 0 None -81 2 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 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]2CCNCN2C1=O 10.1021/jm00169a001
10278394 212962 0 None -1202 2 Human 5.3 pKi = 5.3 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 495 10 0 6 5.7 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCN1CCN(C)CC1 10.1021/jm010544r
CHEMBL86384 212962 0 None -1202 2 Human 5.3 pKi = 5.3 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 495 10 0 6 5.7 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCN1CCN(C)CC1 10.1021/jm010544r
44351337 178494 0 None - 1 Pig 6.3 pKi = 6.3 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 840 10 7 10 2.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL446683 178494 0 None - 1 Pig 6.3 pKi = 6.3 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 840 10 7 10 2.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
54584266 67957 0 None -7585 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1145 20 12 15 0.2 CC(C)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](CCCCNC(=O)c2ccccc2N)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
CHEMBL1765664 67957 0 None -7585 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1145 20 12 15 0.2 CC(C)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](CCCCNC(=O)c2ccccc2N)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
16051933 144908 4 None -25 8 Human 8.3 pKi = 8.3 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=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 10.1021/jm030611c
CHEMBL376685 144908 4 None -25 8 Human 8.3 pKi = 8.3 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=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 10.1021/jm030611c
DB00035 144908 4 None -25 8 Human 8.3 pKi = 8.3 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=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 10.1021/jm030611c
9849525 118203 0 None 61 2 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL327365 118203 0 None 61 2 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325558 119346 0 None 1096 2 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1cccc(O)c1 10.1016/j.bmcl.2004.03.083
CHEMBL330094 119346 0 None 1096 2 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1cccc(O)c1 10.1016/j.bmcl.2004.03.083
44317966 162431 0 None - 1 Pig 8.3 pKi = 8.3 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1124 21 11 14 -0.7 CCOc1ccc(C[C@H]2NC(=O)CC(CC)(CC)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00162a001
CHEMBL404820 162431 0 None - 1 Pig 8.3 pKi = 8.3 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1124 21 11 14 -0.7 CCOc1ccc(C[C@H]2NC(=O)CC(CC)(CC)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00162a001
44520855 186153 0 None 5 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 561 5 1 5 5.9 Cc1cccc(CNC(=O)/C=C2/c3ccccc3N(C(=O)c3ccc(-n4ccc(C)n4)cc3Cl)CCC2(F)F)n1 10.1016/j.bmc.2009.03.001
CHEMBL473872 186153 0 None 5 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 561 5 1 5 5.9 Cc1cccc(CNC(=O)/C=C2/c3ccccc3N(C(=O)c3ccc(-n4ccc(C)n4)cc3Cl)CCC2(F)F)n1 10.1016/j.bmc.2009.03.001
CHEMBL2370640 216682 0 None -1 2 Pig 8.3 pKi = 8.3 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL None None None CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
71457081 89150 0 None 64 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1309 24 5 14 10.2 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
71482251 89150 0 None 64 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1309 24 5 14 10.2 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
CHEMBL2172289 89150 0 None 64 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1309 24 5 14 10.2 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
44294573 168878 0 None -3 2 Pig 8.2 pKi = 8.2 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 953 16 9 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL416114 168878 0 None -3 2 Pig 8.2 pKi = 8.2 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 953 16 9 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44294573 168878 0 None -3 2 Pig 8.2 pKi = 8.2 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 953 16 9 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL416114 168878 0 None -3 2 Pig 8.2 pKi = 8.2 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 953 16 9 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL2369839 216483 0 None -33 4 Human 7.3 pKi = 7.3 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
3537 10776 22 None 3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/acs.jmedchem.8b00697
5311500 10776 22 None 3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/acs.jmedchem.8b00697
CHEMBL363910 10776 22 None 3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/acs.jmedchem.8b00697
3537 10776 22 None 3 3 Human 7.3 pKi = 7.3 Binding
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
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/jm901084f
5311500 10776 22 None 3 3 Human 7.3 pKi = 7.3 Binding
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
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/jm901084f
CHEMBL363910 10776 22 None 3 3 Human 7.3 pKi = 7.3 Binding
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
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/jm901084f
44243143 23796 0 None -8 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 372 5 0 6 4.3 COc1ccc(-n2c(C)nnc2-c2ccc(-c3ccccc3OC)cc2)cn1 10.1021/jm901812z
CHEMBL1254297 23796 0 None -8 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 372 5 0 6 4.3 COc1ccc(-n2c(C)nnc2-c2ccc(-c3ccccc3OC)cc2)cn1 10.1021/jm901812z
CHEMBL2372928 217095 0 None -10 2 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 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]2CCCCN2C1=O 10.1021/jm00169a001
11488952 84359 0 None -2511 3 Human 5.3 pKi = 5.3 Binding
Displacement of vasopressin from human V2RDisplacement of vasopressin from human V2R
ChEMBL 501 7 2 4 4.2 CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)NC(C)C)c1ccc2occc2c1 10.1021/jm060073e
CHEMBL208787 84359 0 None -2511 3 Human 5.3 pKi = 5.3 Binding
Displacement of vasopressin from human V2RDisplacement of vasopressin from human V2R
ChEMBL 501 7 2 4 4.2 CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)NC(C)C)c1ccc2occc2c1 10.1021/jm060073e
5306925 170858 13 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 285 1 0 1 4.3 O=C(c1ccc(Cl)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
CHEMBL4209421 170858 13 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 285 1 0 1 4.3 O=C(c1ccc(Cl)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
16109441 144173 0 None -114 4 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1026 19 12 15 -2.8 NCCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
CHEMBL375323 144173 0 None -114 4 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1026 19 12 15 -2.8 NCCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
168288721 198173 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 532 8 1 4 6.4 CN(C)CCCN1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc21 10.1021/acs.jmedchem.2c00567
CHEMBL5192496 198173 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 532 8 1 4 6.4 CN(C)CCCN1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc21 10.1021/acs.jmedchem.2c00567
145970757 171564 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 307 4 0 1 5.0 CCCCc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/acs.jmedchem.8b00697
CHEMBL4218211 171564 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 307 4 0 1 5.0 CCCCc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/acs.jmedchem.8b00697
44335343 114247 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 519 3 1 3 6.6 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(CC4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(02)00649-2
CHEMBL318392 114247 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 519 3 1 3 6.6 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(CC4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(02)00649-2
54581307 67958 0 None -4073 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1097 21 12 15 -1.4 CC(C)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](CCCCNC(=O)CCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
CHEMBL1765666 67958 0 None -4073 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1097 21 12 15 -1.4 CC(C)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](CCCCNC(=O)CCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
44520869 193713 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 527 6 1 5 4.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCN(C)C)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL490049 193713 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 527 6 1 5 4.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCN(C)C)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
46890440 14123 0 None -173 2 Human 7.3 pKi = 7.3 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 381 2 0 1 6.4 Cc1ccccc1-c1ccc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)c(Cl)c1 10.1016/j.bmcl.2010.04.068
CHEMBL1086272 14123 0 None -173 2 Human 7.3 pKi = 7.3 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 381 2 0 1 6.4 Cc1ccccc1-c1ccc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)c(Cl)c1 10.1016/j.bmcl.2010.04.068
137642420 164839 0 None -11 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@H](O)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL4086079 164839 0 None -11 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@H](O)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.7b00422
71451752 89154 0 None 9 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1295 30 4 17 7.6 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NCCOCCOCCOCCn4cc(CNC(=O)CCC(=O)NC5CCCN(C(=O)c6ccc(NC(=O)c7ccccc7C)cc6)c6ccccc65)nn4)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2172293 89154 0 None 9 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1295 30 4 17 7.6 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NCCOCCOCCOCCn4cc(CNC(=O)CCC(=O)NC5CCCN(C(=O)c6ccc(NC(=O)c7ccccc7C)cc6)c6ccccc65)nn4)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL1790546 215675 0 None -85 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 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]2CCC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
2241 8999 1 None -208 4 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL None None None None 10.1021/jm00169a001
9810632 8999 1 None -208 4 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL None None None None 10.1021/jm00169a001
CHEMBL127686 8999 1 None -208 4 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL None None None None 10.1021/jm00169a001
168280173 197562 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 516 7 1 5 4.7 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00567
CHEMBL5183482 197562 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 516 7 1 5 4.7 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00567
CHEMBL1790551 215679 0 None -229 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 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]2C[C@@H](CN(C)C)C=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
CHEMBL292579 217665 0 None -32 2 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 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]2CCNCN2C1=O 10.1021/jm00169a001
44316236 212304 0 None -23 4 Human 6.3 pKi = 6.3 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 997 16 12 14 -4.0 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H]1CCCN1C(=O)[C@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)NCC(=O)N[C@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
CHEMBL80877 212304 0 None -23 4 Human 6.3 pKi = 6.3 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 997 16 12 14 -4.0 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H]1CCCN1C(=O)[C@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)NCC(=O)N[C@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
46890654 13903 0 None -707 2 Human 6.3 pKi = 6.3 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 377 3 0 2 5.7 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccc(C)cc1 10.1016/j.bmcl.2010.04.068
CHEMBL1085299 13903 0 None -707 2 Human 6.3 pKi = 6.3 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 377 3 0 2 5.7 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccc(C)cc1 10.1016/j.bmcl.2010.04.068
162676461 190291 0 None -707 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 394 3 0 5 4.9 Clc1ccc2c(c1)CCCc1nnc([C@H]3CC[C@H](Oc4ccccn4)CC3)n1-2 10.1021/acs.jmedchem.1c00863
CHEMBL4799793 190291 0 None -707 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 394 3 0 5 4.9 Clc1ccc2c(c1)CCCc1nnc([C@H]3CC[C@H](Oc4ccccn4)CC3)n1-2 10.1021/acs.jmedchem.1c00863
162676461 190291 0 None -707 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]AVP from human V2a receptor expressed in 1132N1 cells assessed as dissociation constant by radioligand binding assayDisplacement of [3H]AVP from human V2a receptor expressed in 1132N1 cells assessed as dissociation constant by radioligand binding assay
ChEMBL 394 3 0 5 4.9 Clc1ccc2c(c1)CCCc1nnc([C@H]3CC[C@H](Oc4ccccn4)CC3)n1-2 10.1016/j.bmcl.2020.127417
CHEMBL4799793 190291 0 None -707 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]AVP from human V2a receptor expressed in 1132N1 cells assessed as dissociation constant by radioligand binding assayDisplacement of [3H]AVP from human V2a receptor expressed in 1132N1 cells assessed as dissociation constant by radioligand binding assay
ChEMBL 394 3 0 5 4.9 Clc1ccc2c(c1)CCCc1nnc([C@H]3CC[C@H](Oc4ccccn4)CC3)n1-2 10.1016/j.bmcl.2020.127417
9981665 125255 4 None -15 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 459 5 2 4 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CC(=O)O)C2 10.1021/jm901812z
CHEMBL341339 125255 4 None -15 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 459 5 2 4 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CC(=O)O)C2 10.1021/jm901812z
CHEMBL2369834 216478 0 None -43 4 Human 6.3 pKi = 6.3 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None NCC[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](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
CHEMBL1790547 215676 0 None -57 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 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]2C=CC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
57519947 80425 0 None -100 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation countingDisplacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 707 9 0 6 4.3 CS(=O)(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)CCc5ccccc54)CC3)c(OC/C=C\I)c2)CC1 10.1016/j.bmc.2012.02.019
CHEMBL2017868 80425 0 None -100 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation countingDisplacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 707 9 0 6 4.3 CS(=O)(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)CCc5ccccc54)CC3)c(OC/C=C\I)c2)CC1 10.1016/j.bmc.2012.02.019
10187283 212992 0 None -194 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 543 7 0 6 5.9 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCc1ccc(C(=O)N2CCN(C)CC2)cc1 10.1021/jm010544r
CHEMBL86577 212992 0 None -194 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 543 7 0 6 5.9 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCc1ccc(C(=O)N2CCN(C)CC2)cc1 10.1021/jm010544r
2249 9008 18 None -162 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to human V2 receptorBinding affinity to human V2 receptor
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1016/j.bmcl.2012.10.116
9872389 9008 18 None -162 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to human V2 receptorBinding affinity to human V2 receptor
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1016/j.bmcl.2012.10.116
CHEMBL1253853 9008 18 None -162 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to human V2 receptorBinding affinity to human V2 receptor
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1016/j.bmcl.2012.10.116
2249 9008 18 None -162 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1021/jm901812z
9872389 9008 18 None -162 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1021/jm901812z
CHEMBL1253853 9008 18 None -162 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1021/jm901812z
44520877 19383 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 547 5 1 5 5.6 Cc1ccnn1-c1ccc(C(=O)N2CCC(F)(F)/C(=C\C(=O)NCc3ccccn3)c3ccccc32)c(Cl)c1 10.1016/j.bmc.2008.09.039
CHEMBL1186990 19383 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 547 5 1 5 5.6 Cc1ccnn1-c1ccc(C(=O)N2CCC(F)(F)/C(=C\C(=O)NCc3ccccn3)c3ccccc32)c(Cl)c1 10.1016/j.bmc.2008.09.039
CHEMBL485761 19383 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 547 5 1 5 5.6 Cc1ccnn1-c1ccc(C(=O)N2CCC(F)(F)/C(=C\C(=O)NCc3ccccn3)c3ccccc32)c(Cl)c1 10.1016/j.bmc.2008.09.039
44351441 103653 0 None -1 2 Pig 8.2 pKi = 8.2 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 1050 16 9 12 1.5 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCN=C(N)N)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL265591 103653 0 None -1 2 Pig 8.2 pKi = 8.2 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 1050 16 9 12 1.5 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCN=C(N)N)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44294575 88889 0 None - 1 Pig 8.2 pKi = 8.2 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00162a001
CHEMBL216606 88889 0 None - 1 Pig 8.2 pKi = 8.2 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00162a001
135916059 207868 0 None 5 3 Human 8.2 pKi = 8.2 Binding
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
ChEMBL 513 4 2 5 6.6 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm901084f
CHEMBL602872 207868 0 None 5 3 Human 8.2 pKi = 8.2 Binding
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
ChEMBL 513 4 2 5 6.6 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm901084f
44294575 88889 0 None - 1 Pig 8.2 pKi = 8.2 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL216606 88889 0 None - 1 Pig 8.2 pKi = 8.2 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
44351278 124060 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidney
ChEMBL 924 15 8 11 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL339532 124060 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidney
ChEMBL 924 15 8 11 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44351278 124060 0 None -1 2 Pig 8.2 pKi = 8.2 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 924 15 8 11 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL339532 124060 0 None -1 2 Pig 8.2 pKi = 8.2 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 924 15 8 11 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44294532 162543 0 None - 1 Pig 8.2 pKi = 8.2 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 910 15 8 11 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL405818 162543 0 None - 1 Pig 8.2 pKi = 8.2 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 910 15 8 11 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
168268939 196693 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 560 7 2 5 5.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5169868 196693 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 560 7 2 5 5.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
44325915 119515 0 None 104 2 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 509 3 1 4 5.6 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2004.03.083
CHEMBL330494 119515 0 None 104 2 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 509 3 1 4 5.6 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2004.03.083
46890186 14025 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 451 2 0 1 7.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3cccc4ccccc34)c(Cl)c2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1085850 14025 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 451 2 0 1 7.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3cccc4ccccc34)c(Cl)c2Cl)C1 10.1016/j.bmcl.2010.04.068
46890709 13609 0 None -6025 2 Human 6.2 pKi = 6.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 402 3 1 2 5.9 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1c[nH]c2ccccc12 10.1016/j.bmcl.2010.04.068
CHEMBL1084008 13609 0 None -6025 2 Human 6.2 pKi = 6.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 402 3 1 2 5.9 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1c[nH]c2ccccc12 10.1016/j.bmcl.2010.04.068
16109437 91079 0 None -316 5 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1065 18 11 14 -0.6 NCCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
CHEMBL221485 91079 0 None -316 5 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1065 18 11 14 -0.6 NCCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
2042 9757 58 None -63 8 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL None None None None 10.1021/jm00171a003
2174 9757 58 None -63 8 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL None None None None 10.1021/jm00171a003
2176 9757 58 None -63 8 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL None None None None 10.1021/jm00171a003
439302 9757 58 None -63 8 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL None None None None 10.1021/jm00171a003
CHEMBL395429 9757 58 None -63 8 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL None None None None 10.1021/jm00171a003
DB00107 9757 58 None -63 8 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL None None None None 10.1021/jm00171a003
168281109 197923 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 512 7 1 5 4.8 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1 10.1021/acs.jmedchem.2c00567
CHEMBL5188374 197923 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 512 7 1 5 4.8 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1 10.1021/acs.jmedchem.2c00567
54584476 69146 0 None -478 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation counting
ChEMBL 630 8 1 10 2.3 COc1ccc(S(=O)(=O)N2C(=O)[C@@](c3cccnc3OC)(N3C[C@H](O)C[C@H]3C(=O)N(C)C)c3cc(Cl)ccc32)c(OC)c1 10.1016/j.bmcl.2011.03.012
CHEMBL1779400 69146 0 None -478 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation counting
ChEMBL 630 8 1 10 2.3 COc1ccc(S(=O)(=O)N2C(=O)[C@@](c3cccnc3OC)(N3C[C@H](O)C[C@H]3C(=O)N(C)C)c3cc(Cl)ccc32)c(OC)c1 10.1016/j.bmcl.2011.03.012
CHEMBL2369842 216486 0 None -41 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
46890052 13627 0 None -11 2 Human 7.2 pKi = 7.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 413 3 0 2 6.6 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc2ccccc12 10.1016/j.bmcl.2010.04.068
CHEMBL1084111 13627 0 None -11 2 Human 7.2 pKi = 7.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 413 3 0 2 6.6 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc2ccccc12 10.1016/j.bmcl.2010.04.068
2239 7863 1 None -501 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]oxytocin from human V2 vasopressin receptorDisplacement of [3H]oxytocin from human V2 vasopressin receptor
ChEMBL 497 7 2 3 3.7 CC(C[C@@H]1C(=O)N[C@@H](C(=O)N1[C@H](c1ccc(cc1F)F)C(=O)NC(C)C)C1Cc2c(C1)cccc2)C 10.1021/jm050557v
6918854 7863 1 None -501 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]oxytocin from human V2 vasopressin receptorDisplacement of [3H]oxytocin from human V2 vasopressin receptor
ChEMBL 497 7 2 3 3.7 CC(C[C@@H]1C(=O)N[C@@H](C(=O)N1[C@H](c1ccc(cc1F)F)C(=O)NC(C)C)C1Cc2c(C1)cccc2)C 10.1021/jm050557v
CHEMBL196478 7863 1 None -501 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]oxytocin from human V2 vasopressin receptorDisplacement of [3H]oxytocin from human V2 vasopressin receptor
ChEMBL 497 7 2 3 3.7 CC(C[C@@H]1C(=O)N[C@@H](C(=O)N1[C@H](c1ccc(cc1F)F)C(=O)NC(C)C)C1Cc2c(C1)cccc2)C 10.1021/jm050557v
2239 7863 1 None -501 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 497 7 2 3 3.7 CC(C[C@@H]1C(=O)N[C@@H](C(=O)N1[C@H](c1ccc(cc1F)F)C(=O)NC(C)C)C1Cc2c(C1)cccc2)C 10.1021/jm901812z
6918854 7863 1 None -501 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 497 7 2 3 3.7 CC(C[C@@H]1C(=O)N[C@@H](C(=O)N1[C@H](c1ccc(cc1F)F)C(=O)NC(C)C)C1Cc2c(C1)cccc2)C 10.1021/jm901812z
CHEMBL196478 7863 1 None -501 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 497 7 2 3 3.7 CC(C[C@@H]1C(=O)N[C@@H](C(=O)N1[C@H](c1ccc(cc1F)F)C(=O)NC(C)C)C1Cc2c(C1)cccc2)C 10.1021/jm901812z
54585429 69150 0 None -112 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation counting
ChEMBL 661 9 1 12 1.7 COc1ccc(S(=O)(=O)N2C(=O)[C@@](c3cnc(OC)nc3OC)(N3C[C@H](O)C[C@H]3C(=O)N(C)C)c3cc(Cl)ccc32)c(OC)c1 10.1016/j.bmcl.2011.03.012
CHEMBL1779404 69150 0 None -112 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation counting
ChEMBL 661 9 1 12 1.7 COc1ccc(S(=O)(=O)N2C(=O)[C@@](c3cnc(OC)nc3OC)(N3C[C@H](O)C[C@H]3C(=O)N(C)C)c3cc(Cl)ccc32)c(OC)c1 10.1016/j.bmcl.2011.03.012
168277442 197290 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 566 7 1 5 5.8 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.2c00567
CHEMBL5179419 197290 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 566 7 1 5 5.8 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.2c00567
168271930 196863 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 530 7 1 5 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1 10.1021/acs.jmedchem.2c00567
CHEMBL5172734 196863 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 530 7 1 5 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1 10.1021/acs.jmedchem.2c00567
53349364 173468 0 None -8 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHO cell membranes after 60 minsDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHO cell membranes after 60 mins
ChEMBL 427 3 1 3 4.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC(=O)N(C)c3cccc(C)c32)cc1 10.1039/C8MD00033F
CHEMBL4282161 173468 0 None -8 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHO cell membranes after 60 minsDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHO cell membranes after 60 mins
ChEMBL 427 3 1 3 4.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC(=O)N(C)c3cccc(C)c32)cc1 10.1039/C8MD00033F
168282729 197837 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 516 7 1 5 4.7 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1F 10.1021/acs.jmedchem.2c00567
CHEMBL5187312 197837 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 516 7 1 5 4.7 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1F 10.1021/acs.jmedchem.2c00567
44325896 214590 0 None 27 2 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 551 4 1 5 4.9 O=C(Nc1ccc(C(=O)N2CC3CS(=O)(=O)CCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL96255 214590 0 None 27 2 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 551 4 1 5 4.9 O=C(Nc1ccc(C(=O)N2CC3CS(=O)(=O)CCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
168287130 198354 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 498 7 1 5 4.5 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1 10.1021/acs.jmedchem.2c00567
CHEMBL5195053 198354 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 498 7 1 5 4.5 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1 10.1021/acs.jmedchem.2c00567
10907482 213054 0 None -724 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 523 10 0 6 5.6 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCC(=O)N1CCN(C)CC1 10.1021/jm010544r
CHEMBL86936 213054 0 None -724 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 523 10 0 6 5.6 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCC(=O)N1CCN(C)CC1 10.1021/jm010544r
100915923 197423 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 558 8 1 4 6.9 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
CHEMBL5181341 197423 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 558 8 1 4 6.9 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
54584265 67956 0 None -12882 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1026 18 11 14 -0.9 CC(C)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](CCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
CHEMBL1765663 67956 0 None -12882 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1026 18 11 14 -0.9 CC(C)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](CCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
46890656 13907 0 None -177 2 Human 6.2 pKi = 6.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 403 3 0 3 6.1 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1coc2ccccc12 10.1016/j.bmcl.2010.04.068
CHEMBL1085301 13907 0 None -177 2 Human 6.2 pKi = 6.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 403 3 0 3 6.1 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1coc2ccccc12 10.1016/j.bmcl.2010.04.068
CHEMBL1790542 215673 0 None -346 2 Rat 5.2 pKi = 5.2 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 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]2CCC(=O)NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
44419027 168561 6 None 1 3 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1053 19 13 15 -4.4 N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2cccnc2)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 10.1021/jm060928n
CHEMBL414074 168561 6 None 1 3 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1053 19 13 15 -4.4 N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2cccnc2)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 10.1021/jm060928n
10206901 213136 0 None -501 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 494 11 0 5 7.3 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCCCC1 10.1021/jm010544r
CHEMBL87455 213136 0 None -501 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 494 11 0 5 7.3 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCCCC1 10.1021/jm010544r
11740743 20880 0 None 1 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to vasopressin V2 receptorBinding affinity to vasopressin V2 receptor
ChEMBL 384 3 1 2 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm3006146
CHEMBL119793 20880 0 None 1 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to vasopressin V2 receptorBinding affinity to vasopressin V2 receptor
ChEMBL 384 3 1 2 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm3006146
44294592 103533 0 None - 1 Pig 8.1 pKi = 8.1 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1007 16 8 12 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@@H]3C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL264540 103533 0 None - 1 Pig 8.1 pKi = 8.1 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1007 16 8 12 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@@H]3C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
44520859 178408 0 None 2 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 572 5 1 6 5.5 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccc(C#N)n4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL446566 178408 0 None 2 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 572 5 1 6 5.5 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccc(C#N)n4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
10411308 208013 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to vasopressin V2 receptorBinding affinity to vasopressin V2 receptor
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm3006146
CHEMBL603708 208013 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to vasopressin V2 receptorBinding affinity to vasopressin V2 receptor
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm3006146
10715974 18694 0 None -4 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 400 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3ccccc32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL118271 18694 0 None -4 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 400 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3ccccc32)cc1 10.1021/acs.jmedchem.7b00422
71449932 89161 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1100 19 3 10 10.4 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NCCCCC(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6-c6ccccc6)cc5)c5ccccc54)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2172391 89161 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1100 19 3 10 10.4 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NCCCCC(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6-c6ccccc6)cc5)c5ccccc54)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2370641 216683 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidney
ChEMBL None None None CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)NCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
56665480 69982 0 None -91 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 754 6 2 8 3.5 CC[C@@H](C)[C@@H]1/N=C(\S)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
CHEMBL1790544 69982 0 None -91 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 754 6 2 8 3.5 CC[C@@H](C)[C@@H]1/N=C(\S)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
CHEMBL2371441 216826 0 None - 1 Pig 5.2 pKi = 5.2 Binding
Inhibition of LVP-sensitive adenylate cyclase in a pig renal medullary preparationInhibition of LVP-sensitive adenylate cyclase in a pig renal medullary preparation
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00399a009
46890571 14129 0 None -177 2 Human 6.2 pKi = 6.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 377 3 0 2 5.7 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc(C)c1 10.1016/j.bmcl.2010.04.068
CHEMBL1086293 14129 0 None -177 2 Human 6.2 pKi = 6.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 377 3 0 2 5.7 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc(C)c1 10.1016/j.bmcl.2010.04.068
47177176 171609 1 None -1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 329 1 0 1 4.4 O=C(c1ccc(Br)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
CHEMBL4218739 171609 1 None -1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 329 1 0 1 4.4 O=C(c1ccc(Br)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
44314222 211539 0 None -8 2 Rat 7.1 pKi = 7.1 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 560 11 1 6 5.1 Cc1ccc(N(C)C(=O)c2ccc(NC(=O)c3ccoc3C)cc2)c(OCCCCCC(=O)N2CCN(C)CC2)c1 10.1016/s0960-894x(01)00723-5
CHEMBL74593 211539 0 None -8 2 Rat 7.1 pKi = 7.1 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 560 11 1 6 5.1 Cc1ccc(N(C)C(=O)c2ccc(NC(=O)c3ccoc3C)cc2)c(OCCCCCC(=O)N2CCN(C)CC2)c1 10.1016/s0960-894x(01)00723-5
CHEMBL1790546 215675 0 None -85 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 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]2CCC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
11144861 113771 0 None -954 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 452 8 1 5 6.1 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCC1CCNCC1 10.1021/jm010544r
CHEMBL315232 113771 0 None -954 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 452 8 1 5 6.1 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCC1CCNCC1 10.1021/jm010544r
CHEMBL1790552 215680 0 None -1 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 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]2CCCN(C)N2C(=O)[C@H]2CCCN(C)N2C1=O 10.1021/jm00171a003
44419028 103684 17 None -630 8 Human 6.1 pKi = 6.1 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1093 18 12 14 -1.6 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
CHEMBL265858 103684 17 None -630 8 Human 6.1 pKi = 6.1 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1093 18 12 14 -1.6 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
44275525 201645 0 None -107151 4 Human 5.1 pKi = 5.1 Binding
The inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorThe inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1525 36 12 20 1.8 CN(C)c1ccc2c(c1)Oc1cc(N(C)C)ccc1C21OC(=O)c2cc(C(=O)N(C(=O)[C@@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccc(O)cc3)N(C)C(=O)CCc3ccc(O)cc3)[C@@H](CCCCN)C(N)=O)ccc21 10.1021/jm9804782
91931055 201645 0 None -107151 4 Human 5.1 pKi = 5.1 Binding
The inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorThe inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1525 36 12 20 1.8 CN(C)c1ccc2c(c1)Oc1cc(N(C)C)ccc1C21OC(=O)c2cc(C(=O)N(C(=O)[C@@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccc(O)cc3)N(C)C(=O)CCc3ccc(O)cc3)[C@@H](CCCCN)C(N)=O)ccc21 10.1021/jm9804782
CHEMBL540192 201645 0 None -107151 4 Human 5.1 pKi = 5.1 Binding
The inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorThe inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1525 36 12 20 1.8 CN(C)c1ccc2c(c1)Oc1cc(N(C)C)ccc1C21OC(=O)c2cc(C(=O)N(C(=O)[C@@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccc(O)cc3)N(C)C(=O)CCc3ccc(O)cc3)[C@@H](CCCCN)C(N)=O)ccc21 10.1021/jm9804782
16109447 90126 0 None -83 4 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1012 18 12 15 -3.2 NCCC[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](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL219272 90126 0 None -83 4 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1012 18 12 15 -3.2 NCCC[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](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
46890100 14074 0 None -33 2 Human 6.1 pKi = 6.1 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 414 3 0 3 6.0 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc2ncccc12 10.1016/j.bmcl.2010.04.068
CHEMBL1086069 14074 0 None -33 2 Human 6.1 pKi = 6.1 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 414 3 0 3 6.0 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc2ncccc12 10.1016/j.bmcl.2010.04.068
67839485 170980 0 None -33 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 327 2 0 1 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
CHEMBL4210854 170980 0 None -33 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 327 2 0 1 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
44520848 206723 0 None 2 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 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 10.1016/j.bmc.2009.10.038
CHEMBL594953 206723 0 None 2 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 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 10.1016/j.bmc.2009.10.038
CHEMBL1790543 215674 0 None -61 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 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]2CCC(=O)NN2C(=O)[C@H]2CCCNN2C1=O 10.1021/jm00171a003
44314343 109830 0 None -134 2 Rat 6.1 pKi = 6.1 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 650 13 1 7 6.0 CCc1nccn1-c1ccccc1C(=O)Nc1ccc(C(=O)N(C)c2ccc(C)cc2OCCCCCC(=O)N2CCN(C)CC2)cc1 10.1016/s0960-894x(01)00723-5
CHEMBL307269 109830 0 None -134 2 Rat 6.1 pKi = 6.1 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 650 13 1 7 6.0 CCc1nccn1-c1ccccc1C(=O)Nc1ccc(C(=O)N(C)c2ccc(C)cc2OCCCCCC(=O)N2CCN(C)CC2)cc1 10.1016/s0960-894x(01)00723-5
44325804 214089 0 None 37 2 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 533 4 1 4 6.5 Cc1ccc2c(c1)N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)CC1CSCCN1C2 10.1016/j.bmcl.2004.03.083
CHEMBL93366 214089 0 None 37 2 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 533 4 1 4 6.5 Cc1ccc2c(c1)N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)CC1CSCCN1C2 10.1016/j.bmcl.2004.03.083
44297516 168070 0 None -37 3 Rat 8.1 pKi = 8.1 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1315 37 15 16 -2.2 CN(C(=O)Cc1ccc(N=[N+]=[N-])cc1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
CHEMBL412192 168070 0 None -37 3 Rat 8.1 pKi = 8.1 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1315 37 15 16 -2.2 CN(C(=O)Cc1ccc(N=[N+]=[N-])cc1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
15416418 163918 0 None -8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 400 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@@H](O)c3ccccc32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL4075127 163918 0 None -8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 400 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@@H](O)c3ccccc32)cc1 10.1021/acs.jmedchem.7b00422
44351439 165806 0 None - 1 Pig 8.1 pKi = 8.1 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 1022 16 8 12 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL409667 165806 0 None - 1 Pig 8.1 pKi = 8.1 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 1022 16 8 12 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44317762 168096 0 None - 1 Pig 8.1 pKi = 8.1 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1067 19 10 13 0.2 CCOc1ccc(C[C@H]2NC(=O)CC(CC)(CC)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00162a001
CHEMBL412392 168096 0 None - 1 Pig 8.1 pKi = 8.1 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1067 19 10 13 0.2 CCOc1ccc(C[C@H]2NC(=O)CC(CC)(CC)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00162a001
CHEMBL2369840 216484 0 None -10 4 Human 7.1 pKi = 7.1 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL None None None NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
10873853 113773 0 None -147 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 438 7 1 5 5.7 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCC1CCNCC1 10.1021/jm010544r
CHEMBL315251 113773 0 None -147 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 438 7 1 5 5.7 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCC1CCNCC1 10.1021/jm010544r
46890262 13458 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 562 3 0 2 9.6 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3cc(Cl)c(-c4cccc5cccnc45)cc3Cl)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1083480 13458 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 562 3 0 2 9.6 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3cc(Cl)c(-c4cccc5cccnc45)cc3Cl)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
46890487 13670 0 None -4 2 Human 7.1 pKi = 7.1 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 377 3 0 2 5.7 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccccc1C 10.1016/j.bmcl.2010.04.068
CHEMBL1084307 13670 0 None -4 2 Human 7.1 pKi = 7.1 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 377 3 0 2 5.7 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccccc1C 10.1016/j.bmcl.2010.04.068
2241 8999 1 None -208 4 Rat 6.1 pKi = 6.1 Binding
Binding affinity towards rat kidney V2 receptor was determined using [3H]arginine vasopressin as radioligandBinding affinity towards rat kidney V2 receptor was determined using [3H]arginine vasopressin as radioligand
ChEMBL None None None None 10.1021/jm00099a019
9810632 8999 1 None -208 4 Rat 6.1 pKi = 6.1 Binding
Binding affinity towards rat kidney V2 receptor was determined using [3H]arginine vasopressin as radioligandBinding affinity towards rat kidney V2 receptor was determined using [3H]arginine vasopressin as radioligand
ChEMBL None None None None 10.1021/jm00099a019
CHEMBL127686 8999 1 None -208 4 Rat 6.1 pKi = 6.1 Binding
Binding affinity towards rat kidney V2 receptor was determined using [3H]arginine vasopressin as radioligandBinding affinity towards rat kidney V2 receptor was determined using [3H]arginine vasopressin as radioligand
ChEMBL None None None None 10.1021/jm00099a019
118734336 125378 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 418 3 1 3 4.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[S@@+]([O-])c3ccccc32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416770 125378 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 418 3 1 3 4.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[S@@+]([O-])c3ccccc32)cc1 10.1021/acs.jmedchem.5b00289
46890531 13509 0 None -38 2 Human 6.1 pKi = 6.1 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 455 5 0 3 7.2 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccccc1Oc1ccccc1 10.1016/j.bmcl.2010.04.068
CHEMBL1083732 13509 0 None -38 2 Human 6.1 pKi = 6.1 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 455 5 0 3 7.2 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccccc1Oc1ccccc1 10.1016/j.bmcl.2010.04.068
10144208 113905 0 None -1047 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 557 7 0 6 6.2 Cc1cccc(OCc2ccc(C(=O)N3CCN(C)CC3)cc2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
CHEMBL316093 113905 0 None -1047 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 557 7 0 6 6.2 Cc1cccc(OCc2ccc(C(=O)N3CCN(C)CC3)cc2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
19607875 125377 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 418 3 1 3 4.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[S+]([O-])c3ccccc32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416769 125377 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 418 3 1 3 4.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[S+]([O-])c3ccccc32)cc1 10.1021/acs.jmedchem.5b00289
73350823 109307 0 None -575 9 Human 5.1 pKi = 5.1 Binding
Binding affinity to human V2R by competitive binding assayBinding affinity to human V2R by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL2424668 109307 0 None -575 9 Human 5.1 pKi = 5.1 Binding
Binding affinity to human V2R by competitive binding assayBinding affinity to human V2R by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL3040578 109307 0 None -575 9 Human 5.1 pKi = 5.1 Binding
Binding affinity to human V2R by competitive binding assayBinding affinity to human V2R by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
2042 9757 58 None -63 8 Rat 7.1 pKi = 7.1 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL None None None None 10.1021/jm00171a003
2174 9757 58 None -63 8 Rat 7.1 pKi = 7.1 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL None None None None 10.1021/jm00171a003
2176 9757 58 None -63 8 Rat 7.1 pKi = 7.1 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL None None None None 10.1021/jm00171a003
439302 9757 58 None -63 8 Rat 7.1 pKi = 7.1 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL None None None None 10.1021/jm00171a003
CHEMBL395429 9757 58 None -63 8 Rat 7.1 pKi = 7.1 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL None None None None 10.1021/jm00171a003
DB00107 9757 58 None -63 8 Rat 7.1 pKi = 7.1 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL None None None None 10.1021/jm00171a003
118734335 125376 0 None -18 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 416 3 1 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3c(C)cccc32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416768 125376 0 None -18 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 416 3 1 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3c(C)cccc32)cc1 10.1021/acs.jmedchem.5b00289
10165683 112903 0 None -676 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 537 13 0 6 6.9 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCCCN1CCN(C)CC1 10.1021/jm010544r
CHEMBL313451 112903 0 None -676 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 537 13 0 6 6.9 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCCCN1CCN(C)CC1 10.1021/jm010544r
168294720 199248 0 None 16 2 Human 8.1 pKi = 8.1 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 601 9 1 5 6.5 CCN1CCN(CCCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccccc32)CC1 10.1021/acs.jmedchem.2c00567
CHEMBL5208751 199248 0 None 16 2 Human 8.1 pKi = 8.1 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 601 9 1 5 6.5 CCN1CCN(CCCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccccc32)CC1 10.1021/acs.jmedchem.2c00567
10392505 115369 0 None 4 2 Human 8.1 pKi = 8.1 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 539 3 1 3 6.6 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(02)00649-2
CHEMBL320416 115369 0 None 4 2 Human 8.1 pKi = 8.1 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 539 3 1 3 6.6 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(02)00649-2
9915472 176302 0 None 14 2 Human 8.1 pKi = 8.1 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 547 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
CHEMBL443498 176302 0 None 14 2 Human 8.1 pKi = 8.1 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 547 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
44325531 213957 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccc(F)cc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL92470 213957 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccc(F)cc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
71455302 89151 0 None 234 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1441 33 5 17 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
71482380 89151 0 None 234 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1441 33 5 17 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
CHEMBL2172290 89151 0 None 234 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1441 33 5 17 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
44520876 19213 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 561 5 1 5 5.9 Cc1cc(C)n(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
CHEMBL1185998 19213 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 561 5 1 5 5.9 Cc1cc(C)n(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
CHEMBL444956 19213 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 561 5 1 5 5.9 Cc1cc(C)n(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
46890261 13457 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 562 3 0 2 9.6 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3ccc(-c4cccc5cccnc45)c(Cl)c3Cl)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1083479 13457 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 562 3 0 2 9.6 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3ccc(-c4cccc5cccnc45)c(Cl)c3Cl)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
44520872 19382 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 533 5 1 5 5.3 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3cccn3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1186989 19382 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 533 5 1 5 5.3 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3cccn3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL485760 19382 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 533 5 1 5 5.3 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3cccn3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL3037878 217703 0 None - 1 Pig 8.0 pKi = 8.0 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL None None None CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44294507 103269 0 None - 1 Pig 8.0 pKi = 8.0 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1051 17 9 13 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL262499 103269 0 None - 1 Pig 8.0 pKi = 8.0 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1051 17 9 13 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
119369 9384 74 None 1 8 Human 8.0 pKi = 8.0 Binding
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%
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm000108p
2197 9384 74 None 1 8 Human 8.0 pKi = 8.0 Binding
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%
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm000108p
4004 9384 74 None 1 8 Human 8.0 pKi = 8.0 Binding
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%
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm000108p
CHEMBL420762 9384 74 None 1 8 Human 8.0 pKi = 8.0 Binding
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%
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm000108p
119369 9384 74 None 1 8 Human 8.0 pKi = 8.0 Binding
Binding affinity to vasopressin V2 receptorBinding affinity to vasopressin V2 receptor
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm3006146
2197 9384 74 None 1 8 Human 8.0 pKi = 8.0 Binding
Binding affinity to vasopressin V2 receptorBinding affinity to vasopressin V2 receptor
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm3006146
4004 9384 74 None 1 8 Human 8.0 pKi = 8.0 Binding
Binding affinity to vasopressin V2 receptorBinding affinity to vasopressin V2 receptor
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm3006146
CHEMBL420762 9384 74 None 1 8 Human 8.0 pKi = 8.0 Binding
Binding affinity to vasopressin V2 receptorBinding affinity to vasopressin V2 receptor
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm3006146
42629369 188973 0 None 2 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 500 5 2 5 4.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL478283 188973 0 None 2 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 500 5 2 5 4.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
42629369 188973 0 None 2 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 500 5 2 5 4.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.10.038
CHEMBL478283 188973 0 None 2 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 500 5 2 5 4.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.10.038
56682530 69984 0 None -23 4 Human 8.0 pKi = 8 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1053 18 12 14 -2.6 CC[C@H](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](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm030611c
CHEMBL1790575 69984 0 None -23 4 Human 8.0 pKi = 8 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1053 18 12 14 -2.6 CC[C@H](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](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm030611c
172997 9112 57 None 64 2 Human 7.1 pKi = 7.1 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)00649-2
2238 9112 57 None 64 2 Human 7.1 pKi = 7.1 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)00649-2
CHEMBL49429 9112 57 None 64 2 Human 7.1 pKi = 7.1 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)00649-2
DB06666 9112 57 None 64 2 Human 7.1 pKi = 7.1 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)00649-2
CHEMBL5074709 221106 0 None -2951 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL None None None O[C@H]1Cc2cc(Cl)ccc2-n2c(nnc2[C@H]2CC[C@H](Oc3ccccn3)CC2)C1 10.1021/acs.jmedchem.1c00863
2173 9730 13 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-AVP from human V2 receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/acs.jmedchem.8b00697
3038506 9730 13 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-AVP from human V2 receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/acs.jmedchem.8b00697
CHEMBL332447 9730 13 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-AVP from human V2 receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/acs.jmedchem.8b00697
DB05838 9730 13 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-AVP from human V2 receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/acs.jmedchem.8b00697
136961690 125372 0 None -87 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL 412 3 1 6 4.2 Cc1ccn(Cc2ccc(C(=O)N3Cc4cnn(C)c4Nc4ccccc43)cc2C)n1 10.1021/jm501395b
CHEMBL3416757 125372 0 None -87 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL 412 3 1 6 4.2 Cc1ccn(Cc2ccc(C(=O)N3Cc4cnn(C)c4Nc4ccccc43)cc2C)n1 10.1021/jm501395b
135916069 208322 0 None -51 3 Human 6.0 pKi = 6.0 Binding
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
ChEMBL 398 2 1 6 4.1 Cc1ccn(-c2ccc(C(=O)N3Cc4cnn(C)c4Nc4ccccc43)cc2C)n1 10.1021/jm901084f
CHEMBL605373 208322 0 None -51 3 Human 6.0 pKi = 6.0 Binding
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
ChEMBL 398 2 1 6 4.1 Cc1ccn(-c2ccc(C(=O)N3Cc4cnn(C)c4Nc4ccccc43)cc2C)n1 10.1021/jm901084f
CHEMBL2371442 216827 0 None - 1 Pig 5.0 pKi = 5.0 Binding
Inhibition of LVP-sensitive adenylate cyclase in a pig renal medullary preparationInhibition of LVP-sensitive adenylate cyclase in a pig renal medullary preparation
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00399a009
44275524 168072 0 None -53703 4 Human 5.0 pKi = 5.0 Binding
The inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorThe inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1471 34 14 20 1.1 CN(C(=O)CCc1ccc(O)cc1)[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N(C(=O)c1ccc2c(c1)C(=O)OC21c2ccc(O)cc2Oc2cc(O)ccc21)[C@@H](CCCCN)C(N)=O 10.1021/jm9804782
91931053 168072 0 None -53703 4 Human 5.0 pKi = 5.0 Binding
The inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorThe inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1471 34 14 20 1.1 CN(C(=O)CCc1ccc(O)cc1)[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N(C(=O)c1ccc2c(c1)C(=O)OC21c2ccc(O)cc2Oc2cc(O)ccc21)[C@@H](CCCCN)C(N)=O 10.1021/jm9804782
CHEMBL412210 168072 0 None -53703 4 Human 5.0 pKi = 5.0 Binding
The inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorThe inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1471 34 14 20 1.1 CN(C(=O)CCc1ccc(O)cc1)[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N(C(=O)c1ccc2c(c1)C(=O)OC21c2ccc(O)cc2Oc2cc(O)ccc21)[C@@H](CCCCN)C(N)=O 10.1021/jm9804782
56678446 69988 0 None -4466 3 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL 1125 16 13 16 -0.3 CC[C@@H](C)[C@H]1NC(=O)[C@@](C)(c2ccc(O)cc2)NC(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN)C(=O)N[C@H](C(N)=O)c2ccc(O)cc2)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H]([C@@H](C)O)NC1=O 10.1021/jm010526+
CHEMBL1790712 69988 0 None -4466 3 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL 1125 16 13 16 -0.3 CC[C@@H](C)[C@H]1NC(=O)[C@@](C)(c2ccc(O)cc2)NC(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN)C(=O)N[C@H](C(N)=O)c2ccc(O)cc2)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H]([C@@H](C)O)NC1=O 10.1021/jm010526+
15953022 125420 0 None -4677 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-vasopressin from human vasopressin V2 receptor expressed in HEK293 cell membranes after 1 hr by scintillation proximity assayDisplacement of [3H]-vasopressin from human vasopressin V2 receptor expressed in HEK293 cell membranes after 1 hr by scintillation proximity assay
ChEMBL 436 3 0 3 5.7 Cc1c(C(=O)N2CCC3(CC2)OCc2ccccc23)c2ccccc2n1Cc1ccccc1 10.1021/jm501745f
CHEMBL3416860 125420 0 None -4677 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-vasopressin from human vasopressin V2 receptor expressed in HEK293 cell membranes after 1 hr by scintillation proximity assayDisplacement of [3H]-vasopressin from human vasopressin V2 receptor expressed in HEK293 cell membranes after 1 hr by scintillation proximity assay
ChEMBL 436 3 0 3 5.7 Cc1c(C(=O)N2CCC3(CC2)OCc2ccccc23)c2ccccc2n1Cc1ccccc1 10.1021/jm501745f
44314552 211829 0 None -18 2 Rat 7.0 pKi = 7.0 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 628 12 1 6 6.8 Cc1ccc(N(C)C(=O)c2ccc(NC(=O)c3ccoc3C)cc2)c(OCCCCCC(=O)N2CCC(N3CCCCC3)CC2)c1 10.1016/s0960-894x(01)00723-5
CHEMBL77105 211829 0 None -18 2 Rat 7.0 pKi = 7.0 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 628 12 1 6 6.8 Cc1ccc(N(C)C(=O)c2ccc(NC(=O)c3ccoc3C)cc2)c(OCCCCCC(=O)N2CCC(N3CCCCC3)CC2)c1 10.1016/s0960-894x(01)00723-5
11340891 10094 30 None -891 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL 494 6 1 6 2.0 CC[C@@H]([C@@H]1C(=O)N[C@@H](C(=O)N1[C@@H](C(=O)N1CCOCC1)c1coc(n1)C)C1Cc2c(C1)cccc2)C 10.1016/j.bmcl.2007.11.008
8403 10094 30 None -891 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL 494 6 1 6 2.0 CC[C@@H]([C@@H]1C(=O)N[C@@H](C(=O)N1[C@@H](C(=O)N1CCOCC1)c1coc(n1)C)C1Cc2c(C1)cccc2)C 10.1016/j.bmcl.2007.11.008
CHEMBL429736 10094 30 None -891 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL 494 6 1 6 2.0 CC[C@@H]([C@@H]1C(=O)N[C@@H](C(=O)N1[C@@H](C(=O)N1CCOCC1)c1coc(n1)C)C1Cc2c(C1)cccc2)C 10.1016/j.bmcl.2007.11.008
DB11818 10094 30 None -891 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL 494 6 1 6 2.0 CC[C@@H]([C@@H]1C(=O)N[C@@H](C(=O)N1[C@@H](C(=O)N1CCOCC1)c1coc(n1)C)C1Cc2c(C1)cccc2)C 10.1016/j.bmcl.2007.11.008
2253 9012 20 None -12882 6 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue
ChEMBL 586 7 0 7 4.4 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)Cc1ccc[n+](c1C)[O-] 10.1021/jm901812z
5311202 9012 20 None -12882 6 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue
ChEMBL 586 7 0 7 4.4 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)Cc1ccc[n+](c1C)[O-] 10.1021/jm901812z
CHEMBL306645 9012 20 None -12882 6 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue
ChEMBL 586 7 0 7 4.4 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)Cc1ccc[n+](c1C)[O-] 10.1021/jm901812z
10303620 213055 0 None -933 4 Human 6.0 pKi = 6.0 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 577 12 0 6 7.8 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCC(N2CCCCC2)CC1 10.1021/jm010544r
CHEMBL86949 213055 0 None -933 4 Human 6.0 pKi = 6.0 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 577 12 0 6 7.8 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCC(N2CCCCC2)CC1 10.1021/jm010544r
53349471 125381 0 None -22 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 413 3 1 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(C)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416774 125381 0 None -22 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 413 3 1 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(C)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
168297437 199140 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 566 7 1 5 5.8 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1021/acs.jmedchem.2c00567
CHEMBL5207214 199140 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 566 7 1 5 5.8 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1021/acs.jmedchem.2c00567
119369 9384 74 None -1 8 Rat 8.1 pIC50 = 8.1 Binding
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
Drug Central 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
2197 9384 74 None -1 8 Rat 8.1 pIC50 = 8.1 Binding
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
Drug Central 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
4004 9384 74 None -1 8 Rat 8.1 pIC50 = 8.1 Binding
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
Drug Central 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
CHEMBL420762 9384 74 None -1 8 Rat 8.1 pIC50 = 8.1 Binding
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
Drug Central 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
146681949 222856 0 None - 9 Pig 8.1 pIC50 = 8.1 Binding
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
Drug Central 1083 19 14 16 -5.4 C1CC(N(C1)C(=O)C2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N None
146681949 222856 0 None -6 9 Bovine 8.1 pKd = 8.1 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
Drug Central 1083 19 14 16 -5.4 C1CC(N(C1)C(=O)C2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N None
10615 7360 32 None -1288249 4 Human 5.0 pKd = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 31951127
46200932 7360 32 None -1288249 4 Human 5.0 pKd = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 31951127
CHEMBL4297183 7360 32 None -1288249 4 Human 5.0 pKd = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 31951127
DB14823 7360 32 None -1288249 4 Human 5.0 pKd = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 31951127
2042 9757 58 None -831 8 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None None
2174 9757 58 None -831 8 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None None
2176 9757 58 None -831 8 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None None
439302 9757 58 None -831 8 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None None
CHEMBL395429 9757 58 None -831 8 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None None
DB00107 9757 58 None -831 8 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None None
216237 10615 89 3H-AVP 2 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
2226 10615 89 3H-AVP 2 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
4110 10615 89 3H-AVP 2 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
443894 10615 89 3H-AVP 2 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
CHEMBL344159 10615 89 3H-AVP 2 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
DB06212 10615 89 3H-AVP 2 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
151171 7947 50 3H-Oxytocin -2 6 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
216322 7947 50 3H-Oxytocin -2 6 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
2203 7947 50 3H-Oxytocin -2 6 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
732 7947 50 3H-Oxytocin -2 6 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
CHEMBL1755 7947 50 3H-Oxytocin -2 6 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
DB00872 7947 50 3H-Oxytocin -2 6 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
216237 10615 89 3H-AVP 2 5 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
2226 10615 89 3H-AVP 2 5 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
4110 10615 89 3H-AVP 2 5 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
443894 10615 89 3H-AVP 2 5 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
CHEMBL344159 10615 89 3H-AVP 2 5 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
DB06212 10615 89 3H-AVP 2 5 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
146681949 222856 0 3H-Oxytocin -1 9 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 1083 19 14 16 -5.4 C1CC(N(C1)C(=O)C2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N None
146681949 222856 0 3H-AVP -1 9 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 1083 19 14 16 -5.4 C1CC(N(C1)C(=O)C2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N None
146681949 222856 0 3H-AVP -1 9 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 1083 19 14 16 -5.4 C1CC(N(C1)C(=O)C2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N None
216237 10615 89 3H-AVP -2 5 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
2226 10615 89 3H-AVP -2 5 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
4110 10615 89 3H-AVP -2 5 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
443894 10615 89 3H-AVP -2 5 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
CHEMBL344159 10615 89 3H-AVP -2 5 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
DB06212 10615 89 3H-AVP -2 5 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
46783812 222858 0 3H-AVP 6 3 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 1182 19 14 16 -6.7 CC(=O)O.C1CC(N(C1)C(=O)C2CSSCCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N.O.O.O None
None 222857 0 3H-Oxytocin -83 3 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 1151 20 12 15 -2.3 COC1=CC=C(C=C1)CC2C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(CSSC3(CCCCC3)CC(=O)N2)C(=O)N4CCCC4C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N)CC(=O)N)CCC(=O)N)CC5=CC=CC=C5 None
119376 8622 48 3H-VASOPRESSIN -54954 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 8622 48 3H-VASOPRESSIN -54954 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 8622 48 3H-VASOPRESSIN -54954 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
135409468 8816 69 3H-VASOPRESSIN -3548 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 8816 69 3H-VASOPRESSIN -3548 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 8816 69 3H-VASOPRESSIN -3548 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
114904 9728 56 3H-AVP -446 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 449 7 1 4 3.2 CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2c1cccc2 None
114904 9728 56 3H-Oxytocin -446 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 449 7 1 4 3.2 CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2c1cccc2 None
2196 9728 56 3H-AVP -446 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 449 7 1 4 3.2 CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2c1cccc2 None
2196 9728 56 3H-Oxytocin -446 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 449 7 1 4 3.2 CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2c1cccc2 None
CHEMBL296908 9728 56 3H-AVP -446 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 449 7 1 4 3.2 CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2c1cccc2 None
CHEMBL296908 9728 56 3H-Oxytocin -446 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 449 7 1 4 3.2 CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2c1cccc2 None
128563 10237 33 3H-VASOPRESSIN -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 10237 33 3H-VASOPRESSIN -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 10237 33 3H-VASOPRESSIN -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 10237 33 3H-VASOPRESSIN -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
185 10778 60 3H-VASOPRESSIN -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 10778 60 3H-VASOPRESSIN -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 10778 60 3H-VASOPRESSIN -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 10778 60 3H-VASOPRESSIN -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
21830793 98610 10 3H-8-OH-DPAT -66069 46 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 98610 10 3H-8-OH-DPAT -66069 46 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
3663 106743 83 3H-VASOPRESSIN -288 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
CHEMBL286494 106743 83 3H-VASOPRESSIN -288 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
44208932 147485 7 UNDEFINED -89125 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
CHEMBL381689 147485 7 UNDEFINED -89125 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
5280343 195054 124 3H-VASOPRESSIN -147 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 195054 124 3H-VASOPRESSIN -147 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 195054 124 3H-VASOPRESSIN -147 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
5281600 209804 92 3H-VASOPRESSIN -275 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 209804 92 3H-VASOPRESSIN -275 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
1973 210262 15 3H-AVP -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 210262 15 3H-AVP -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 210262 15 3H-AVP -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
4054 212280 72 3H-VASOPRESSIN -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 212280 72 3H-VASOPRESSIN -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 212280 72 3H-VASOPRESSIN -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
None 222772 0 3H-VASOPRESSIN -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 2 0 4 3.6 CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl None
6971132 222788 0 3H-VASOPRESSIN -2570 14 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 268 1 2 2 2.1 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)O None
None 223018 0 3H-VASOPRESSIN -95499 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
None 223090 0 3H-VASOPRESSIN -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 223091 0 3H-VASOPRESSIN -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 223092 0 3H-VASOPRESSIN -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 223093 0 3H-VASOPRESSIN -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 223095 0 3H-VASOPRESSIN -1 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 223096 0 3H-VASOPRESSIN -1 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 223097 0 3H-VASOPRESSIN -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 4 3 4 -1.3 C(CS(=O)(=O)O)C(C(=O)O)N None
None 223106 0 3H-VASOPRESSIN -16 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 536 11 1 4 9.0 CC(C)C(=O)C12C(=O)C(=C(C(C1=O)(CC(C2(C)CCC=C(C)C)CC=C(C)C)CC=C(C)C)O)CC=C(C)C None
4978 223107 0 3H-VASOPRESSIN -7 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 520 1 7 9 4.3 CC1=CC(=C2C3=C1C4=C5C(=C(C=C4CO)O)C(=O)C6=C(C=C(C7=C6C5=C3C8=C7C(=CC(=C8C2=O)O)O)O)O)O None
None 223108 0 3H-VASOPRESSIN -3 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 464 4 8 12 -0.6 C1=CC(=C(C=C1C2=C(C(=C3C(=CC(=O)C=C3O2)O)O)OC4C(C(C(C(O4)CO)O)O)O)O)O None
None 223109 0 3H-VASOPRESSIN -281 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 610 6 10 16 -1.7 CC1C(C(C(C(O1)OCC2C(C(C(C(O2)OC3=C(OC4=CC(=CC(=C4C3=O)O)O)C5=CC(=C(C=C5)O)O)O)O)O)O)O)O None
None 223110 0 3H-VASOPRESSIN -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 448 3 7 11 0.4 CC1C(C(C(C(O1)OC2=C(OC3=CC(=O)C=C(C3=C2O)O)C4=CC(=C(C=C4)O)O)O)O)O None
2042 9757 58 3H-Oxytocin -63 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2174 9757 58 3H-Oxytocin -63 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2176 9757 58 3H-Oxytocin -63 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
439302 9757 58 3H-Oxytocin -63 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL395429 9757 58 3H-Oxytocin -63 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00107 9757 58 3H-Oxytocin -63 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2042 9757 58 3H-AVP -831 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
2174 9757 58 3H-AVP -831 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
2176 9757 58 3H-AVP -831 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
439302 9757 58 3H-AVP -831 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL395429 9757 58 3H-AVP -831 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00107 9757 58 3H-AVP -831 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
None 222963 0 3H-Oxytocin -309 4 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 755 14 5 8 1.7 CC(C=C)C(C(=O)N1CCCCC1(C=O)C(=O)N2CCCCC2)NC(=O)C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCCN5C(=O)C(CC6=CN=CN6)N None
146681949 222856 0 3H-AVP -1 9 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 1083 19 14 16 -5.4 C1CC(N(C1)C(=O)C2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N None
None 222964 0 3H-Oxytocin -64 4 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 780 14 4 9 2.2 CCC(C)C(C(=O)N(C(CC1=CNC2=CC=CC=C21)C=O)C(=O)C3CCCN3C(=O)C(CC4=CC=CCC4(C(=O)N5CCNCC5)C(=O)N6CC=CC=C6)NC)N None
151171 7947 50 3H-AVP -2 6 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
216322 7947 50 3H-AVP -2 6 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
2203 7947 50 3H-AVP -2 6 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
732 7947 50 3H-AVP -2 6 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
CHEMBL1755 7947 50 3H-AVP -2 6 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
DB00872 7947 50 3H-AVP -2 6 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
146681949 222856 0 3H-AVP -1 9 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 1083 19 14 16 -5.4 C1CC(N(C1)C(=O)C2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N None
None 222963 0 3H-Oxytocin -309 4 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 755 14 5 8 1.7 CC(C=C)C(C(=O)N1CCCCC1(C=O)C(=O)N2CCCCC2)NC(=O)C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCCN5C(=O)C(CC6=CN=CN6)N None
None 222965 0 3H-Oxytocin -676 4 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 768 14 3 10 2.3 CCC(C)C(C(=O)C1(CCCN1C(=O)C(CC2=NC(N=C2)(C(=O)N3CCCCC3)C(=O)N4CCCCC4)N)C=O)NC(=O)C(CC5=CC6=CC=CC=C6C=C5)N None
None 222857 0 3H-AVP -83 3 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 1151 20 12 15 -2.3 COC1=CC=C(C=C1)CC2C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(CSSC3(CCCCC3)CC(=O)N2)C(=O)N4CCCC4C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N)CC(=O)N)CCC(=O)N)CC5=CC=CC=C5 None
119369 9384 74 3H-AVP -1 8 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
2197 9384 74 3H-AVP -1 8 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
4004 9384 74 3H-AVP -1 8 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
CHEMBL420762 9384 74 3H-AVP -1 8 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
11169 7584 37 None -1 2 Human 8.3 pKi = 8.3 Binding
vasopressin V2 receptors expressed in COS-7 cellsvasopressin V2 receptors expressed in COS-7 cells
Drug Central 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 None
131676677 7584 37 None -1 2 Human 8.3 pKi = 8.3 Binding
vasopressin V2 receptors expressed in COS-7 cellsvasopressin V2 receptors expressed in COS-7 cells
Drug Central 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 None
165708555 7584 37 None -1 2 Human 8.3 pKi = 8.3 Binding
vasopressin V2 receptors expressed in COS-7 cellsvasopressin V2 receptors expressed in COS-7 cells
Drug Central 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 None
16681432 7584 37 None -1 2 Human 8.3 pKi = 8.3 Binding
vasopressin V2 receptors expressed in COS-7 cellsvasopressin V2 receptors expressed in COS-7 cells
Drug Central 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 None
495 7584 37 None -1 2 Human 8.3 pKi = 8.3 Binding
vasopressin V2 receptors expressed in COS-7 cellsvasopressin V2 receptors expressed in COS-7 cells
Drug Central 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 None
CHEMBL3301668 7584 37 None -1 2 Human 8.3 pKi = 8.3 Binding
vasopressin V2 receptors expressed in COS-7 cellsvasopressin V2 receptors expressed in COS-7 cells
Drug Central 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 None
DB01282 7584 37 None -1 2 Human 8.3 pKi = 8.3 Binding
vasopressin V2 receptors expressed in COS-7 cellsvasopressin V2 receptors expressed in COS-7 cells
Drug Central 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 None
119369 9384 74 3H-Oxytocin -1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
2197 9384 74 3H-Oxytocin -1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
4004 9384 74 3H-Oxytocin -1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
CHEMBL420762 9384 74 3H-Oxytocin -1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
119369 9384 74 3H-AVP -1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
2197 9384 74 3H-AVP -1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
4004 9384 74 3H-AVP -1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
CHEMBL420762 9384 74 3H-AVP -1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
133612094 223265 0 None -13 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
Drug Central 993 18 11 15 -3.0 CCC(C)C1C(=O)NC(C(=O)NC(C(=O)NC(CSSCCC(=O)NC(C(=O)N1)CC2=CC=C(C=C2)OCC)C(=O)N3CCCC3C(=O)NC(CCCN)C(=O)NCC(=O)N)CC(=O)N)C(C)O None
2042 9757 58 3H-AVP -63 8 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase None None None None None
2174 9757 58 3H-AVP -63 8 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase None None None None None
2176 9757 58 3H-AVP -63 8 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase None None None None None
439302 9757 58 3H-AVP -63 8 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL395429 9757 58 3H-AVP -63 8 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00107 9757 58 3H-AVP -63 8 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase None None None None None
2042 9757 58 None -63 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central None None None None None
2174 9757 58 None -63 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central None None None None None
2176 9757 58 None -63 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central None None None None None
439302 9757 58 None -63 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central None None None None None
CHEMBL395429 9757 58 None -63 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central None None None None None
DB00107 9757 58 None -63 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central None None None None None
46783812 222858 0 3H-Oxytocin 6 3 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 1182 19 14 16 -6.7 CC(=O)O.C1CC(N(C1)C(=O)C2CSSCCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N.O.O.O None
119369 9384 74 None 1 8 Human 8.1 pKi = 8.1 Binding
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%
Drug Central 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
2197 9384 74 None 1 8 Human 8.1 pKi = 8.1 Binding
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%
Drug Central 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
4004 9384 74 None 1 8 Human 8.1 pKi = 8.1 Binding
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%
Drug Central 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
CHEMBL420762 9384 74 None 1 8 Human 8.1 pKi = 8.1 Binding
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%
Drug Central 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
122172899 224484 0 None -1 8 Human 8.1 pKi = 8.1 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
Drug Central 1068 19 14 15 -4.1 NC(=O)CC[C@@H]1NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC(=O)CCSSC[C@H](NC(=O)[C@H](CC(N)=O)NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CCCNC(N)=N)C(=O)NCC(N)=O None
151171 7947 50 None -2 6 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
216322 7947 50 None -2 6 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
2203 7947 50 None -2 6 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
732 7947 50 None -2 6 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
CHEMBL1755 7947 50 None -2 6 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
DB00872 7947 50 None -2 6 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
216237 10615 89 None -2 5 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
2226 10615 89 None -2 5 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
4110 10615 89 None -2 5 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
443894 10615 89 None -2 5 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
CHEMBL344159 10615 89 None -2 5 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
DB06212 10615 89 None -2 5 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
146681949 222856 0 None -1 9 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
Drug Central 1083 19 14 16 -5.4 C1CC(N(C1)C(=O)C2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N None
None 222965 0 3H-Oxytocin -676 4 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 768 14 3 10 2.3 CCC(C)C(C(=O)C1(CCCN1C(=O)C(CC2=NC(N=C2)(C(=O)N3CCCCC3)C(=O)N4CCCCC4)N)C=O)NC(=O)C(CC5=CC6=CC=CC=C6C=C5)N None
216237 10615 89 None 2 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
2226 10615 89 None 2 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
4110 10615 89 None 2 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
443894 10615 89 None 2 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
CHEMBL344159 10615 89 None 2 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
DB06212 10615 89 None 2 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
122172899 224484 0 None -1 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
Drug Central 1068 19 14 15 -4.1 NC(=O)CC[C@@H]1NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC(=O)CCSSC[C@H](NC(=O)[C@H](CC(N)=O)NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CCCNC(N)=N)C(=O)NCC(N)=O None
146681949 222856 0 None -1 9 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
Drug Central 1083 19 14 16 -5.4 C1CC(N(C1)C(=O)C2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N None
119369 9384 74 3H-AVP 1 8 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
2197 9384 74 3H-AVP 1 8 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
4004 9384 74 3H-AVP 1 8 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
CHEMBL420762 9384 74 3H-AVP 1 8 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
151171 7947 50 None -1 6 Human 8.0 pKi = 8.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
216322 7947 50 None -1 6 Human 8.0 pKi = 8.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
2203 7947 50 None -1 6 Human 8.0 pKi = 8.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
732 7947 50 None -1 6 Human 8.0 pKi = 8.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
CHEMBL1755 7947 50 None -1 6 Human 8.0 pKi = 8.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
DB00872 7947 50 None -1 6 Human 8.0 pKi = 8.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
133612094 223265 0 3H-AVP -13 5 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 993 18 11 15 -3.0 CCC(C)C1C(=O)NC(C(=O)NC(C(=O)NC(CSSCCC(=O)NC(C(=O)N1)CC2=CC=C(C=C2)OCC)C(=O)N3CCCC3C(=O)NC(CCCN)C(=O)NCC(=O)N)CC(=O)N)C(C)O None
10444 9106 14 None -7 3 Human 5.8 pKi = 5.8 Binding
Binding affinity determined by a TR-FRET binding assay on HEK cells expressing SNAP-tagged V<sub>2</sub> receptors using 20 nM fluorescent DY647 and increasing concentration of competitor.Binding affinity determined by a TR-FRET binding assay on HEK cells expressing SNAP-tagged V<sub>2</sub> receptors using 20 nM fluorescent DY647 and increasing concentration of competitor.
Guide to Pharmacology 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 30199637
139030525 9106 14 None -7 3 Human 5.8 pKi = 5.8 Binding
Binding affinity determined by a TR-FRET binding assay on HEK cells expressing SNAP-tagged V<sub>2</sub> receptors using 20 nM fluorescent DY647 and increasing concentration of competitor.Binding affinity determined by a TR-FRET binding assay on HEK cells expressing SNAP-tagged V<sub>2</sub> receptors using 20 nM fluorescent DY647 and increasing concentration of competitor.
Guide to Pharmacology 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 30199637
145711714 9106 14 None -7 3 Human 5.8 pKi = 5.8 Binding
Binding affinity determined by a TR-FRET binding assay on HEK cells expressing SNAP-tagged V<sub>2</sub> receptors using 20 nM fluorescent DY647 and increasing concentration of competitor.Binding affinity determined by a TR-FRET binding assay on HEK cells expressing SNAP-tagged V<sub>2</sub> receptors using 20 nM fluorescent DY647 and increasing concentration of competitor.
Guide to Pharmacology 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 30199637
CHEMBL4204210 9106 14 None -7 3 Human 5.8 pKi = 5.8 Binding
Binding affinity determined by a TR-FRET binding assay on HEK cells expressing SNAP-tagged V<sub>2</sub> receptors using 20 nM fluorescent DY647 and increasing concentration of competitor.Binding affinity determined by a TR-FRET binding assay on HEK cells expressing SNAP-tagged V<sub>2</sub> receptors using 20 nM fluorescent DY647 and increasing concentration of competitor.
Guide to Pharmacology 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 30199637
2184 8273 0 None -645 3 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2184 8273 0 None -645 3 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1649739
2184 8273 0 None -645 3 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2173 9730 13 None 8 2 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10780976
3038506 9730 13 None 8 2 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10780976
CHEMBL332447 9730 13 None 8 2 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10780976
DB05838 9730 13 None 8 2 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10780976
2236 8128 0 None - 1 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2236 8128 0 None - 1 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
3080966 8128 0 None - 1 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
3080966 8128 0 None - 1 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2172 9170 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2172 9170 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2959 9170 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2959 9170 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
644076 9170 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
644076 9170 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
CHEMBL1200690 9170 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
CHEMBL1200690 9170 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
DB14642 9170 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
DB14642 9170 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
119369 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 11012895
119369 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9322919
119369 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9792651
119369 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9864265
119369 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9884074
2197 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 11012895
2197 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9322919
2197 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9792651
2197 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9864265
2197 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9884074
4004 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 11012895
4004 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9322919
4004 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9792651
4004 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9864265
4004 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9884074
CHEMBL420762 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 11012895
CHEMBL420762 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9322919
CHEMBL420762 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9792651
CHEMBL420762 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9864265
CHEMBL420762 9384 74 None 1 8 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9884074
2181 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
2181 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2181 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
2181 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2181 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
2181 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2181 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2181 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2182 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
2182 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2182 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
2182 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2182 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
2182 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2182 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2182 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
27991 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
27991 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
27991 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
27991 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
27991 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
27991 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
27991 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
27991 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
5311065 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
5311065 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
5311065 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
5311065 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
5311065 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
5311065 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
5311065 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
5311065 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
CHEMBL1429 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
CHEMBL1429 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
CHEMBL1429 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
CHEMBL1429 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
CHEMBL1429 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
CHEMBL1429 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
CHEMBL1429 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
CHEMBL1429 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
CHEMBL264448 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
CHEMBL264448 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
CHEMBL264448 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
CHEMBL264448 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
CHEMBL264448 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
CHEMBL264448 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
CHEMBL264448 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
CHEMBL264448 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
DB00035 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
DB00035 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
DB00035 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
DB00035 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
DB00035 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
DB00035 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
DB00035 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
DB00035 8113 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2169 7254 0 None -31 5 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2169 7254 0 None -31 5 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
68649 7254 0 None -31 5 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
68649 7254 0 None -31 5 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2168 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10519430
2168 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
2168 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2168 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2168 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
2168 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2168 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
2168 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2168 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
2168 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9864265
2168 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2810 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10519430
2810 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
2810 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2810 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2810 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
2810 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2810 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
2810 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2810 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
2810 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9864265
2810 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
644077 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10519430
644077 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
644077 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
644077 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
644077 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
644077 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
644077 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
644077 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
644077 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
644077 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9864265
644077 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
CHEMBL373742 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10519430
CHEMBL373742 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
CHEMBL373742 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
CHEMBL373742 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
CHEMBL373742 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
CHEMBL373742 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
CHEMBL373742 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
CHEMBL373742 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
CHEMBL373742 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
CHEMBL373742 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9864265
CHEMBL373742 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
DB00067 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10519430
DB00067 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
DB00067 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
DB00067 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
DB00067 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
DB00067 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
DB00067 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
DB00067 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
DB00067 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
DB00067 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9864265
DB00067 10748 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
158348 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 10519430
158348 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 11012895
158348 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 8981918
158348 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9792651
158348 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9884074
2199 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 10519430
2199 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 11012895
2199 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 8981918
2199 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9792651
2199 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9884074
CHEMBL4283439 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 10519430
CHEMBL4283439 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 11012895
CHEMBL4283439 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 8981918
CHEMBL4283439 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9792651
CHEMBL4283439 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9884074
DB14923 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 10519430
DB14923 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 11012895
DB14923 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 8981918
DB14923 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9792651
DB14923 10260 18 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9884074
172997 9112 57 None 64 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 11012895
172997 9112 57 None 64 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 9651149
2238 9112 57 None 64 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 11012895
2238 9112 57 None 64 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 9651149
CHEMBL49429 9112 57 None 64 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 11012895
CHEMBL49429 9112 57 None 64 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 9651149
DB06666 9112 57 None 64 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 11012895
DB06666 9112 57 None 64 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 9651149
216237 10615 89 None 2 5 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
2226 10615 89 None 2 5 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
4110 10615 89 None 2 5 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
443894 10615 89 None 2 5 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
CHEMBL344159 10615 89 None 2 5 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
DB06212 10615 89 None 2 5 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
151171 7947 50 None -1 6 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 20471258
216322 7947 50 None -1 6 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 20471258
2203 7947 50 None -1 6 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 20471258
732 7947 50 None -1 6 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 20471258
CHEMBL1755 7947 50 None -1 6 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 20471258
DB00872 7947 50 None -1 6 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 20471258
8529 10127 0 None -30199 3 Human 4.5 pKi > 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 4 0 4 3.9 CN(CCN1CC(c2c1cc(Cl)cc2)C(=O)N1CCC2(CC1)OCc1c2cccc1)C 25654260
91827367 10127 0 None -30199 3 Human 4.5 pKi > 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 4 0 4 3.9 CN(CCN1CC(c2c1cc(Cl)cc2)C(=O)N1CCC2(CC1)OCc1c2cccc1)C 25654260
114904 9728 56 None -1412 7 Human 4.5 pKi None 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 449 7 1 4 3.2 CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2c1cccc2 9322919
2196 9728 56 None -1412 7 Human 4.5 pKi None 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 449 7 1 4 3.2 CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2c1cccc2 9322919
CHEMBL296908 9728 56 None -1412 7 Human 4.5 pKi None 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 449 7 1 4 3.2 CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2c1cccc2 9322919
2222 8135 0 None -794 3 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2209 9864 0 None -707 3 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2213 7306 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
2213 7306 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14722330
3008 7306 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
3008 7306 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14722330
5311010 7306 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
5311010 7306 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14722330
68613 7306 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
68613 7306 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14722330
CHEMBL378642 7306 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
CHEMBL378642 7306 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14722330
CHEMBL382301 7306 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
CHEMBL382301 7306 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14722330
DB09059 7306 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
DB09059 7306 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14722330
2202 9537 33 None -489 5 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 11861823
9895468 9537 33 None -489 5 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 11861823
CHEMBL582857 9537 33 None -489 5 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 11861823
DB12643 9537 33 None -489 5 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 11861823
2221 8137 0 None -3981 4 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2221 8137 0 None -3981 4 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2042 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
2042 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2042 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
2042 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2042 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
2042 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2174 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
2174 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2174 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
2174 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2174 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
2174 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2176 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
2176 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2176 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
2176 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2176 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
2176 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
439302 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
439302 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
439302 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
439302 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
439302 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
439302 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
CHEMBL395429 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
CHEMBL395429 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
CHEMBL395429 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
CHEMBL395429 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
CHEMBL395429 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
CHEMBL395429 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
DB00107 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
DB00107 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
DB00107 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
DB00107 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
DB00107 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
DB00107 9757 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2188 8125 0 None -316 4 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17300166
2186 8124 0 None -630 4 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17300166
2195 9686 0 None -794 3 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2204 10889 5 None -1258 4 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 616 5 1 5 6.4 O=C(N1CCC(CC1)N1CCCCC1)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccoc1C 15661579
9917025 10889 5 None -1258 4 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 616 5 1 5 6.4 O=C(N1CCC(CC1)N1CCCCC1)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccoc1C 15661579
CHEMBL3307200 10889 5 None -1258 4 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 616 5 1 5 6.4 O=C(N1CCC(CC1)N1CCCCC1)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccoc1C 15661579
2187 8123 0 None -707 4 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2210 9865 0 None -398 3 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
119517 8256 0 None -354 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
119517 8256 0 None -354 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2225 8256 0 None -354 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2225 8256 0 None -354 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2208 9863 0 None -281 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2208 9863 0 None -281 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2190 8225 0 None -501 4 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
2189 8226 0 None -630 4 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17300166
2185 8274 0 None -501 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2211 9866 0 None -398 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2219 8136 0 None -199 4 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11337500
2200 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10866830
2200 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 11012895
2200 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 11429400
2200 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 9322919
2200 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 9884074
3482 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10866830
3482 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 11012895
3482 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 11429400
3482 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 9322919
3482 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 9884074
60943 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10866830
60943 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 11012895
60943 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 11429400
60943 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 9322919
60943 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 9884074
CHEMBL419667 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10866830
CHEMBL419667 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 11012895
CHEMBL419667 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 11429400
CHEMBL419667 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 9322919
CHEMBL419667 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 9884074
DB13929 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10866830
DB13929 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 11012895
DB13929 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 11429400
DB13929 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 9322919
DB13929 10084 46 None -177 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 9884074
2223 8134 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10866830
2223 8134 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2223 8134 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
2223 8134 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2223 8134 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
2223 8134 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
6917952 8134 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10866830
6917952 8134 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
6917952 8134 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
6917952 8134 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
6917952 8134 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
6917952 8134 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2235 8129 0 None -31 2 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2191 8227 0 None -630 4 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17300166
2215 8126 0 None -1 3 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
164712 9880 0 None -50 3 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2178 9880 0 None -50 3 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
CHEMBL3272682 9880 0 None -50 3 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2237 8130 0 None -19 2 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2212 10532 0 None -63 3 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2214 8127 0 None -1 3 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2214 8127 0 None -1 3 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2170 8114 0 None -7 3 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2170 8114 0 None -7 3 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
119369 9384 74 None -1 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9792651
119369 9384 74 None -1 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9864265
2197 9384 74 None -1 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9792651
2197 9384 74 None -1 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9864265
4004 9384 74 None -1 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9792651
4004 9384 74 None -1 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9864265
CHEMBL420762 9384 74 None -1 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9792651
CHEMBL420762 9384 74 None -1 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9864265
122322 8132 0 None -8 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
122322 8132 0 None -8 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2217 8132 0 None -8 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2217 8132 0 None -8 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2181 8113 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2181 8113 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
2182 8113 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2182 8113 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
27991 8113 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
27991 8113 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
5311065 8113 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
5311065 8113 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
CHEMBL1429 8113 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
CHEMBL1429 8113 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
CHEMBL264448 8113 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
CHEMBL264448 8113 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
DB00035 8113 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
DB00035 8113 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
2170 8114 0 None 7 3 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2235 8129 0 None 31 2 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
171113 10742 0 None -3 3 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2180 10742 0 None -3 3 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
CHEMBL3274309 10742 0 None -3 3 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2237 8130 0 None 19 2 Rat 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2181 8113 42 None 6 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2182 8113 42 None 6 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
27991 8113 42 None 6 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
5311065 8113 42 None 6 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
CHEMBL1429 8113 42 None 6 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
CHEMBL264448 8113 42 None 6 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
DB00035 8113 42 None 6 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2183 8295 0 None 3 3 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2183 8295 0 None 3 3 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
6441676 8295 0 None 3 3 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
6441676 8295 0 None 3 3 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2229 10383 0 None - 1 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
216237 10615 89 None -2 5 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
2226 10615 89 None -2 5 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
4110 10615 89 None -2 5 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
443894 10615 89 None -2 5 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
CHEMBL344159 10615 89 None -2 5 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
DB06212 10615 89 None -2 5 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
2205 10895 6 None -3 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 11429400
9810140 10895 6 None -3 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 11429400
CHEMBL307483 10895 6 None -3 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 11429400
2198 10193 2 None 46 2 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 537 4 1 4 6.1 Clc1cc(ccc1C(=O)N1C[C@H]2COCCN2Cc2c1cccc2)NC(=O)c1ccccc1c1ccccc1 16620295
9807249 10193 2 None 46 2 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 537 4 1 4 6.1 Clc1cc(ccc1C(=O)N1C[C@H]2COCCN2Cc2c1cccc2)NC(=O)c1ccccc1c1ccccc1 16620295
CHEMBL1192593 10193 2 None 46 2 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 537 4 1 4 6.1 Clc1cc(ccc1C(=O)N1C[C@H]2COCCN2Cc2c1cccc2)NC(=O)c1ccccc1c1ccccc1 16620295
2216 8131 0 None -1 2 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10866830
158348 10260 18 None 2 4 Rat 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9792651
2199 10260 18 None 2 4 Rat 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9792651
CHEMBL4283439 10260 18 None 2 4 Rat 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9792651
DB14923 10260 18 None 2 4 Rat 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9792651