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
2168 3913 35 None 3 6 Rat 10.2 pEC50 = 10.2 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
2810 3913 35 None 3 6 Rat 10.2 pEC50 = 10.2 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
644077 3913 35 None 3 6 Rat 10.2 pEC50 = 10.2 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
CHEMBL373742 3913 35 None 3 6 Rat 10.2 pEC50 = 10.2 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
DB00067 3913 35 None 3 6 Rat 10.2 pEC50 = 10.2 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
2168 3913 35 None 3 6 Rat 10.2 pEC50 = 10.2 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
2810 3913 35 None 3 6 Rat 10.2 pEC50 = 10.2 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
644077 3913 35 None 3 6 Rat 10.2 pEC50 = 10.2 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
CHEMBL373742 3913 35 None 3 6 Rat 10.2 pEC50 = 10.2 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
DB00067 3913 35 None 3 6 Rat 10.2 pEC50 = 10.2 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
CHEMBL1819441 207270 0 None 1 4 Rat 10.2 pEC50 = 10.2 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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 207270 0 None 1 4 Rat 10.1 pEC50 = 10.1 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
CHEMBL1817706 207244 0 None 2 5 Rat 10.0 pEC50 = 10 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
CHEMBL1817706 207244 0 None 2 5 Rat 10.0 pEC50 = 10.0 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
CHEMBL1819542 207273 10 None 2 4 Rat 9.9 pEC50 = 9.9 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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 207273 10 None 2 4 Rat 9.9 pEC50 = 9.9 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
CHEMBL1817704 207242 0 None 2 5 Rat 9.9 pEC50 = 9.9 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
90285421 114484 0 None 9 2 Human 9.9 pEC50 = 9.9 Functional
Antagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assayAntagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assay
ChEMBL 334 4 1 5 2.7 O=S(=O)(Nc1ccnn1-c1ccccn1)c1ccc(Cl)cc1 10.1016/j.ejmech.2017.05.013
CHEMBL3342789 114484 0 None 9 2 Human 9.9 pEC50 = 9.9 Functional
Antagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assayAntagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assay
ChEMBL 334 4 1 5 2.7 O=S(=O)(Nc1ccnn1-c1ccccn1)c1ccc(Cl)cc1 10.1016/j.ejmech.2017.05.013
3601935 161813 2 None -1 2 Human 9.9 pEC50 = 9.9 Functional
Antagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assayAntagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assay
ChEMBL 271 3 1 4 1.9 Cn1nccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.ejmech.2017.05.013
CHEMBL4165132 161813 2 None -1 2 Human 9.9 pEC50 = 9.9 Functional
Antagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assayAntagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assay
ChEMBL 271 3 1 4 1.9 Cn1nccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.ejmech.2017.05.013
CHEMBL1817704 207242 0 None 2 5 Rat 9.9 pEC50 = 9.9 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
CHEMBL1819540 207271 0 None 64 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 207271 0 None 64 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1819441 207270 0 None -1 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 207270 0 None -1 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
76685194 114485 0 None 5 2 Human 9.8 pEC50 = 9.8 Functional
Antagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assayAntagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assay
ChEMBL 368 4 1 5 3.1 O=S(=O)(Nc1ccnn1-c1ccccn1)c1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2017.05.013
CHEMBL3342790 114485 0 None 5 2 Human 9.8 pEC50 = 9.8 Functional
Antagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assayAntagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assay
ChEMBL 368 4 1 5 3.1 O=S(=O)(Nc1ccnn1-c1ccccn1)c1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2017.05.013
5014150 162305 1 None -1 2 Human 9.8 pEC50 = 9.8 Functional
Antagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assayAntagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assay
ChEMBL 305 3 1 4 2.2 Cn1nccc1NS(=O)(=O)c1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2017.05.013
CHEMBL4173036 162305 1 None -1 2 Human 9.8 pEC50 = 9.8 Functional
Antagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assayAntagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assay
ChEMBL 305 3 1 4 2.2 Cn1nccc1NS(=O)(=O)c1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2017.05.013
CHEMBL1817707 207245 0 None 3 5 Rat 9.8 pEC50 = 9.8 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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 207245 0 None 3 5 Rat 9.8 pEC50 = 9.8 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
2042 2935 52 None -3 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human V1A receptor expressed in HEK293 cells assessed as intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric methodAgonist activity at human V1A receptor expressed in HEK293 cells assessed as intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method
ChEMBL None None None None 10.1016/j.bmc.2019.06.018
2174 2935 52 None -3 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human V1A receptor expressed in HEK293 cells assessed as intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric methodAgonist activity at human V1A receptor expressed in HEK293 cells assessed as intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method
ChEMBL None None None None 10.1016/j.bmc.2019.06.018
2176 2935 52 None -3 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human V1A receptor expressed in HEK293 cells assessed as intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric methodAgonist activity at human V1A receptor expressed in HEK293 cells assessed as intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method
ChEMBL None None None None 10.1016/j.bmc.2019.06.018
439302 2935 52 None -3 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human V1A receptor expressed in HEK293 cells assessed as intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric methodAgonist activity at human V1A receptor expressed in HEK293 cells assessed as intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method
ChEMBL None None None None 10.1016/j.bmc.2019.06.018
CHEMBL395429 2935 52 None -3 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human V1A receptor expressed in HEK293 cells assessed as intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric methodAgonist activity at human V1A receptor expressed in HEK293 cells assessed as intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method
ChEMBL None None None None 10.1016/j.bmc.2019.06.018
DB00107 2935 52 None -3 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human V1A receptor expressed in HEK293 cells assessed as intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric methodAgonist activity at human V1A receptor expressed in HEK293 cells assessed as intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method
ChEMBL None None None None 10.1016/j.bmc.2019.06.018
CHEMBL1817706 207244 0 None -2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817706 207244 0 None -2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1819541 207272 0 None 14 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
2168 3913 35 None -3 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
2810 3913 35 None -3 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
644077 3913 35 None -3 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
CHEMBL373742 3913 35 None -3 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
DB00067 3913 35 None -3 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
CHEMBL1819541 207272 0 None 14 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
2168 3913 35 None -3 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
2810 3913 35 None -3 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
644077 3913 35 None -3 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
CHEMBL373742 3913 35 None -3 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
DB00067 3913 35 None -3 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
CHEMBL1819555 207285 0 None 8 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 207285 0 None 8 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817705 207243 0 None 1 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 207243 0 None 1 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1819542 207273 10 None -2 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 207273 10 None -2 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817705 207243 0 None -1 5 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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 207243 0 None -1 5 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
CHEMBL1817761 207257 0 None 2 5 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
CHEMBL1817761 207257 0 None 2 5 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
CHEMBL1817702 207240 0 None 2 4 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
CHEMBL1817702 207240 0 None 2 4 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
CHEMBL1819440 207269 19 None 1 5 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
CHEMBL1819440 207269 19 None 1 5 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
CHEMBL1817704 207242 0 None -2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817704 207242 0 None -2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1819543 207274 0 None 18 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1819543 207274 0 None 18 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1819548 207279 0 None 53 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
56672274 64447 0 None - 1 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1063 20 13 16 -5.1 CCC(N)C(=O)NCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](O)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
CHEMBL1819439 64447 0 None - 1 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1063 20 13 16 -5.1 CCC(N)C(=O)NCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](O)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
CHEMBL1819548 207279 0 None 53 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
56672274 64447 0 None - 1 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1063 20 13 16 -5.1 CCC(N)C(=O)NCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](O)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
CHEMBL1819439 64447 0 None - 1 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1063 20 13 16 -5.1 CCC(N)C(=O)NCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](O)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
11454 3521 9 None 4 5 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
53330936 3521 9 None 4 5 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
CHEMBL1817709 3521 9 None 4 5 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
DB12495 3521 9 None 4 5 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
11454 3521 9 None 4 5 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
53330936 3521 9 None 4 5 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
CHEMBL1817709 3521 9 None 4 5 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
DB12495 3521 9 None 4 5 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
CHEMBL1817707 207245 0 None -3 5 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 207245 0 None -3 5 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1819549 207280 0 None 47 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 207280 0 None 47 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817756 207252 0 None 4 5 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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 207252 0 None 4 5 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
CHEMBL1817761 207257 0 None -2 5 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1819440 207269 19 None -1 5 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817761 207257 0 None -2 5 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1819440 207269 19 None -1 5 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1819554 207284 0 None 5 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1819554 207284 0 None 5 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817708 207246 0 None 53 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817708 207246 0 None 53 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817702 207240 0 None -2 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817702 207240 0 None -2 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1819556 207286 0 None 67 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 207286 0 None 67 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817754 207250 0 None 7 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm200278m
CHEMBL1817754 207250 0 None 7 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm200278m
53362258 64293 0 None 1 3 Rat 9.0 pEC50 = 9 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1005 17 11 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](CC(=O)N(C)C)NC1=O 10.1021/jm200278m
CHEMBL1817695 64293 0 None 1 3 Rat 9.0 pEC50 = 9 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1005 17 11 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](CC(=O)N(C)C)NC1=O 10.1021/jm200278m
53362155 64472 0 None 25 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 64472 0 None 25 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
53362155 64472 0 None 25 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 64472 0 None 25 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817752 207248 0 None 77 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817692 207239 0 None 5 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817752 207248 0 None 77 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 207266 0 None 40 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 207266 0 None 40 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817692 207239 0 None 5 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817755 207251 0 None 20 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm200278m
CHEMBL1817755 207251 0 None 20 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm200278m
CHEMBL1817772 207268 0 None 11 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817772 207268 0 None 11 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
53362258 64293 0 None -1 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1005 17 11 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](CC(=O)N(C)C)NC1=O 10.1021/jm200278m
CHEMBL1817695 64293 0 None -1 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1005 17 11 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](CC(=O)N(C)C)NC1=O 10.1021/jm200278m
53362258 64293 0 None -1 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1005 17 11 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](CC(=O)N(C)C)NC1=O 10.1021/jm200278m
CHEMBL1817695 64293 0 None -1 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1005 17 11 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](CC(=O)N(C)C)NC1=O 10.1021/jm200278m
CHEMBL1817749 207247 0 None 1 3 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817757 207253 0 None 52 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817769 207265 0 None 7 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1819552 207282 0 None 3 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
2369069 178704 7 None -1 3 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 346 3 0 5 4.0 CCN1C(=S)SC(=O)C1=C1C=C(C)N(Cc2ccco2)C(C)=C1 nan
CHEMBL473106 178704 7 None -1 3 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 346 3 0 5 4.0 CCN1C(=S)SC(=O)C1=C1C=C(C)N(Cc2ccco2)C(C)=C1 nan
CHEMBL1817769 207265 0 None 7 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1819552 207282 0 None 3 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817762 207258 0 None 43 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
53362202 64290 0 None 5 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 64290 0 None 5 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
25161471 54754 14 None 1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 265 4 2 2 3.5 Oc1ccc(Cl)cc1CNCc1ccc(F)cc1 nan
CHEMBL1356933 54754 14 None 1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 265 4 2 2 3.5 Oc1ccc(Cl)cc1CNCc1ccc(F)cc1 nan
CHEMBL1616435 54754 14 None 1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 265 4 2 2 3.5 Oc1ccc(Cl)cc1CNCc1ccc(F)cc1 nan
53362202 64290 0 None 5 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 64290 0 None 5 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817762 207258 0 None 43 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817767 207263 0 None 10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817767 207263 0 None 10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1819553 207283 0 None 19 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
5329098 98123 75 None -1 3 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 238 1 2 1 3.1 Cc1cc(C)c(/C=C2\C(=O)Nc3ccccc32)[nH]1 nan
CHEMBL276711 98123 75 None -1 3 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 238 1 2 1 3.1 Cc1cc(C)c(/C=C2\C(=O)Nc3ccccc32)[nH]1 nan
2919564 29988 18 None 1 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 404 9 2 5 4.0 COc1ccc(CCNCC(O)Cn2c3ccccc3c3ccccc32)cc1OC nan
CHEMBL1390471 29988 18 None 1 2 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 404 9 2 5 4.0 COc1ccc(CCNCC(O)Cn2c3ccccc3c3ccccc32)cc1OC nan
CHEMBL1819553 207283 0 None 19 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817763 207259 0 None 19 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817759 207255 0 None 31 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817763 207259 0 None 19 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817759 207255 0 None 31 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817760 207256 0 None 14 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817758 207254 0 None 63 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817760 207256 0 None 14 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817758 207254 0 None 63 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
1112934 55802 8 None -1 3 Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 425 5 1 5 4.7 N=c1n(CC(=O)c2ccc(Br)s2)c2ccccc2n1Cc1ccccc1 nan
CHEMBL1587205 55802 8 None -1 3 Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 425 5 1 5 4.7 N=c1n(CC(=O)c2ccc(Br)s2)c2ccccc2n1Cc1ccccc1 nan
CHEMBL1625302 55802 8 None -1 3 Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 425 5 1 5 4.7 N=c1n(CC(=O)c2ccc(Br)s2)c2ccccc2n1Cc1ccccc1 nan
53362312 64297 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1051 20 14 17 -6.0 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)NC(CO)CO)NC1=O 10.1021/jm200278m
CHEMBL1817699 64297 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1051 20 14 17 -6.0 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)NC(CO)CO)NC1=O 10.1021/jm200278m
53362312 64297 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1051 20 14 17 -6.0 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)NC(CO)CO)NC1=O 10.1021/jm200278m
CHEMBL1817699 64297 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1051 20 14 17 -6.0 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)NC(CO)CO)NC1=O 10.1021/jm200278m
42601352 35175 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 282 4 2 3 3.4 Oc1ccc(Cl)cc1CNCc1ccc(Cl)nc1 nan
CHEMBL1437791 35175 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 282 4 2 3 3.4 Oc1ccc(Cl)cc1CNCc1ccc(Cl)nc1 nan
CHEMBL3211384 35175 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 282 4 2 3 3.4 Oc1ccc(Cl)cc1CNCc1ccc(Cl)nc1 nan
CHEMBL1817671 207238 0 None 53 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 207238 0 None 53 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1819547 207278 0 None 22 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
6174589 107100 5 None 1 2 Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 379 6 2 6 2.0 CCN(CC)c1ccc2cc(C(N)=O)/c(=N\NC(=O)c3ccncc3)oc2c1 nan
CHEMBL3189462 107100 5 None 1 2 Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 379 6 2 6 2.0 CCN(CC)c1ccc2cc(C(N)=O)/c(=N\NC(=O)c3ccncc3)oc2c1 nan
CHEMBL1819547 207278 0 None 22 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817749 207247 0 None 1 3 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
53362311 64296 0 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1035 20 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)NCCCO)NC1=O 10.1021/jm200278m
CHEMBL1817698 64296 0 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1035 20 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)NCCCO)NC1=O 10.1021/jm200278m
CHEMBL1819555 207285 0 None -8 4 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
53362311 64296 0 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1035 20 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)NCCCO)NC1=O 10.1021/jm200278m
CHEMBL1817698 64296 0 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1035 20 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)NCCCO)NC1=O 10.1021/jm200278m
CHEMBL1819555 207285 0 None -8 4 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
CHEMBL1819550 207281 0 None 47 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 207281 0 None 47 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
11454 3521 9 None -4 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
53330936 3521 9 None -4 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
CHEMBL1817709 3521 9 None -4 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
DB12495 3521 9 None -4 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
CHEMBL1817753 207249 0 None 26 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
11454 3521 9 None -4 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
53330936 3521 9 None -4 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
CHEMBL1817709 3521 9 None -4 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
DB12495 3521 9 None -4 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None None 10.1021/jm200278m
CHEMBL1817753 207249 0 None 26 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817756 207252 0 None -4 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 207252 0 None -4 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
53362548 64302 0 None 1 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 64302 0 None 1 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
53362548 64302 0 None 1 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 64302 0 None 1 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
53362311 64296 0 None -1 3 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1035 20 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)NCCCO)NC1=O 10.1021/jm200278m
CHEMBL1817698 64296 0 None -1 3 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1035 20 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)NCCCO)NC1=O 10.1021/jm200278m
53362311 64296 0 None -1 3 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1035 20 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)NCCCO)NC1=O 10.1021/jm200278m
CHEMBL1817698 64296 0 None -1 3 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1035 20 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)NCCCO)NC1=O 10.1021/jm200278m
CHEMBL1817749 207247 0 None -1 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817749 207247 0 None -1 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
53362154 64471 0 None 7 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 64471 0 None 7 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
3650228 55694 6 None 1 2 Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 402 5 2 3 5.1 COc1ccc(C2NCCc3c2[nH]c2ccccc32)cc1COc1ccc(F)cc1 nan
CHEMBL1549574 55694 6 None 1 2 Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 402 5 2 3 5.1 COc1ccc(C2NCCc3c2[nH]c2ccccc32)cc1COc1ccc(F)cc1 nan
CHEMBL1624349 55694 6 None 1 2 Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 402 5 2 3 5.1 COc1ccc(C2NCCc3c2[nH]c2ccccc32)cc1COc1ccc(F)cc1 nan
53362154 64471 0 None 7 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 64471 0 None 7 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
215028 54985 3 None 1 2 Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 330 1 1 3 4.0 Clc1ccc2c(c1)C(N1CCNCC1)Cc1ccccc1S2 nan
CHEMBL1339676 54985 3 None 1 2 Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 330 1 1 3 4.0 Clc1ccc2c(c1)C(N1CCNCC1)Cc1ccccc1S2 nan
CHEMBL1618211 54985 3 None 1 2 Human 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 330 1 1 3 4.0 Clc1ccc2c(c1)C(N1CCNCC1)Cc1ccccc1S2 nan
23983726 48583 1 None 1 2 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 472 1 3 3 6.2 CC1(C)CC[C@@]2(C(=O)O)C(C1)C1=CCC3[C@@]4(C)CC[C@H](O)C(C)(C)C4CC[C@@]3(C)[C@]1(C)C[C@H]2O nan
CHEMBL1559201 48583 1 None 1 2 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434991 (Counterscreen (V1R agonists in triplicate)), 2482 (Summary (OXTR agonists)), 434963 (Confirmation screen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 472 1 3 3 6.2 CC1(C)CC[C@@]2(C(=O)O)C(C1)C1=CCC3[C@@]4(C)CC[C@H](O)C(C)(C)C4CC[C@@]3(C)[C@]1(C)C[C@H]2O nan
2042 2935 52 None -3 5 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human V1a receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V1a 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 2935 52 None -3 5 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human V1a receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V1a 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 2935 52 None -3 5 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human V1a receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V1a 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 2935 52 None -3 5 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human V1a receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V1a 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 2935 52 None -3 5 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human V1a receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V1a 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 2935 52 None -3 5 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human V1a receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V1a 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
CHEMBL1817703 207241 0 None 7 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1819545 207276 0 None 6 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccnc2)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
CHEMBL1817771 207267 0 None 44 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817771 207267 0 None 44 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
53362204 64291 0 None 10 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 991 17 12 15 -4.8 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)NC)NC1=O 10.1021/jm200278m
CHEMBL1817693 64291 0 None 10 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 991 17 12 15 -4.8 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)NC)NC1=O 10.1021/jm200278m
53362204 64291 0 None 10 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 991 17 12 15 -4.8 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)NC)NC1=O 10.1021/jm200278m
CHEMBL1817693 64291 0 None 10 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 991 17 12 15 -4.8 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)NC)NC1=O 10.1021/jm200278m
53362547 64301 0 None 2 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 64301 0 None 2 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 64301 0 None 2 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 64301 0 None 2 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817703 207241 0 None 7 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1819545 207276 0 None 6 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccnc2)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
53363017 64470 0 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 64470 0 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
53363017 64470 0 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 64470 0 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
53362259 64294 0 None 13 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 64294 0 None 13 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
53362259 64294 0 None 13 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 64294 0 None 13 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1819554 207284 0 None -5 4 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
CHEMBL1819554 207284 0 None -5 4 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
53362369 64300 0 None 8 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1065 22 13 17 -5.4 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](CC(=O)NCCOCCO)NC1=O 10.1021/jm200278m
CHEMBL1817701 64300 0 None 8 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1065 22 13 17 -5.4 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](CC(=O)NCCOCCO)NC1=O 10.1021/jm200278m
53362548 64302 0 None -1 4 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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 64302 0 None -1 4 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
53362369 64300 0 None 8 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1065 22 13 17 -5.4 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](CC(=O)NCCOCCO)NC1=O 10.1021/jm200278m
CHEMBL1817701 64300 0 None 8 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1065 22 13 17 -5.4 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](CC(=O)NCCOCCO)NC1=O 10.1021/jm200278m
53362548 64302 0 None -1 4 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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 64302 0 None -1 4 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
449224 168409 9 None -208 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at vasopressin 1a receptor (unknown origin)Agonist activity at vasopressin 1a receptor (unknown origin)
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 10.1016/j.bmcl.2017.12.027
CHEMBL439044 168409 9 None -208 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at vasopressin 1a receptor (unknown origin)Agonist activity at vasopressin 1a receptor (unknown origin)
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 10.1016/j.bmcl.2017.12.027
3385342 39906 7 None - 1 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 384 6 2 5 3.2 CC(NC(=O)Nc1ccc([N+](=O)[O-])cc1)C(c1ccccc1)N1CCOCC1 nan
CHEMBL1479813 39906 7 None - 1 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 384 6 2 5 3.2 CC(NC(=O)Nc1ccc([N+](=O)[O-])cc1)C(c1ccccc1)N1CCOCC1 nan
2871994 41447 15 None - 1 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 324 3 1 4 2.4 O=C1c2cccc3c(N4CCCCC4)ccc(c23)C(=O)N1CCO nan
CHEMBL1492232 41447 15 None - 1 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 324 3 1 4 2.4 O=C1c2cccc3c(N4CCCCC4)ccc(c23)C(=O)N1CCO nan
53362368 64299 0 None 5 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1035 19 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)NCC(C)O)NC1=O 10.1021/jm200278m
CHEMBL1817700 64299 0 None 5 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1035 19 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)NCC(C)O)NC1=O 10.1021/jm200278m
53362368 64299 0 None 5 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1035 19 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)NCC(C)O)NC1=O 10.1021/jm200278m
CHEMBL1817700 64299 0 None 5 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1035 19 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)NCC(C)O)NC1=O 10.1021/jm200278m
53362257 64292 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1005 18 12 15 -4.4 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](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817694 64292 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1005 18 12 15 -4.4 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](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
53362257 64292 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1005 18 12 15 -4.4 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](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817694 64292 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1005 18 12 15 -4.4 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](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1819544 207275 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cnc[nH]2)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
CHEMBL1819544 207275 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cnc[nH]2)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
CHEMBL1817770 207266 0 None -40 4 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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 207266 0 None -40 4 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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
53363016 64469 0 None 9 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 64469 0 None 9 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
53363016 64469 0 None 9 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 64469 0 None 9 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
3484134 51477 6 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 407 5 2 3 4.6 CC(NC(=O)Nc1ccc(Cl)c(Cl)c1)C(c1ccccc1)N1CCOCC1 nan
CHEMBL1584768 51477 6 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 407 5 2 3 4.6 CC(NC(=O)Nc1ccc(Cl)c(Cl)c1)C(c1ccccc1)N1CCOCC1 nan
1471100 24213 13 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 350 1 1 4 3.7 O=c1c2cc(Br)ccc2nc(-c2cccc(Cl)c2)n1O nan
CHEMBL1341433 24213 13 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 350 1 1 4 3.7 O=c1c2cc(Br)ccc2nc(-c2cccc(Cl)c2)n1O nan
53362156 64289 0 None 7 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 64289 0 None 7 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
53362156 64289 0 None 7 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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 64289 0 None 7 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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
CHEMBL1817764 207260 0 None 47 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817764 207260 0 None 47 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817765 207261 0 None 51 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817765 207261 0 None 51 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817768 207264 0 None 15 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
2042 2935 52 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at vasopressin 1a receptor (unknown origin)Agonist activity at vasopressin 1a receptor (unknown origin)
ChEMBL None None None None 10.1016/j.bmcl.2017.12.027
2174 2935 52 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at vasopressin 1a receptor (unknown origin)Agonist activity at vasopressin 1a receptor (unknown origin)
ChEMBL None None None None 10.1016/j.bmcl.2017.12.027
2176 2935 52 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at vasopressin 1a receptor (unknown origin)Agonist activity at vasopressin 1a receptor (unknown origin)
ChEMBL None None None None 10.1016/j.bmcl.2017.12.027
439302 2935 52 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at vasopressin 1a receptor (unknown origin)Agonist activity at vasopressin 1a receptor (unknown origin)
ChEMBL None None None None 10.1016/j.bmcl.2017.12.027
CHEMBL395429 2935 52 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at vasopressin 1a receptor (unknown origin)Agonist activity at vasopressin 1a receptor (unknown origin)
ChEMBL None None None None 10.1016/j.bmcl.2017.12.027
DB00107 2935 52 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at vasopressin 1a receptor (unknown origin)Agonist activity at vasopressin 1a receptor (unknown origin)
ChEMBL None None None None 10.1016/j.bmcl.2017.12.027
CHEMBL1817768 207264 0 None 15 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817766 207262 0 None 13 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
53362310 64295 0 None 3 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1021 19 13 16 -5.4 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](CC(=O)NCCO)NC1=O 10.1021/jm200278m
CHEMBL1817697 64295 0 None 3 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1021 19 13 16 -5.4 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](CC(=O)NCCO)NC1=O 10.1021/jm200278m
CHEMBL1817766 207262 0 None 13 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a 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](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817754 207250 0 None -7 3 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm200278m
53362310 64295 0 None 3 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1021 19 13 16 -5.4 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](CC(=O)NCCO)NC1=O 10.1021/jm200278m
CHEMBL1817697 64295 0 None 3 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1021 19 13 16 -5.4 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](CC(=O)NCCO)NC1=O 10.1021/jm200278m
CHEMBL1817754 207250 0 None -7 3 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm200278m
CHEMBL1817692 207239 0 None -5 3 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817692 207239 0 None -5 3 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant rat vasopressin V1a 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](CC(N)=O)NC1=O 10.1021/jm200278m
25163004 72572 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 1317 54 6 22 6.4 C#CCOCCOCCOCCNc1nc(N2CCN(C(=O)CCCCCCCCCCNC(=O)[C@H](CCCCN)n3cc(C[C@@H](C)CC)nn3)CC2)nc(N2CCN(C(=O)CCCCCCCCCCNC(=O)[C@@H](CCC(=O)O)n3cc(CCCCCN)nn3)CC2)n1 nan
CHEMBL2004487 72572 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). (Class of assay: confirmatory) [Related pubchem assays: 2435 (Primary screen (OXTR agonists in singlicate)), 434964 (Confirmation screen (V1R agonists in triplicate)), 434969 (Counterscreen (OXTR agonists in triplicate)), 2797 (Counterscreen (V1R agonists in singlicate))]
ChEMBL 1317 54 6 22 6.4 C#CCOCCOCCOCCNc1nc(N2CCN(C(=O)CCCCCCCCCCNC(=O)[C@H](CCCCN)n3cc(C[C@@H](C)CC)nn3)CC2)nc(N2CCN(C(=O)CCCCCCCCCCNC(=O)[C@@H](CCC(=O)O)n3cc(CCCCCN)nn3)CC2)n1 nan
2042 2935 52 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human liver vasopressin V1a 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 liver vasopressin V1a 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 2935 52 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human liver vasopressin V1a 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 liver vasopressin V1a 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 2935 52 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human liver vasopressin V1a 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 liver vasopressin V1a 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 2935 52 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human liver vasopressin V1a 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 liver vasopressin V1a 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 2935 52 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human liver vasopressin V1a 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 liver vasopressin V1a 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 2935 52 None -3 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human liver vasopressin V1a 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 liver vasopressin V1a 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
9935206 65731 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 487 4 0 7 2.8 CN(C)S(=O)(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
CHEMBL1837039 65731 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 487 4 0 7 2.8 CN(C)S(=O)(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
162676461 182930 0 None - 1 Human 9.0 pIC50 = 9 Functional
Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate readerInhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader
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 182930 0 None - 1 Human 9.0 pIC50 = 9 Functional
Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate readerInhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader
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 182930 0 None - 1 Human 9.0 pIC50 = 9 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium 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 182930 0 None - 1 Human 9.0 pIC50 = 9 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium 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
CHEMBL5070261 212458 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate readerInhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader
ChEMBL None None None OC1Cc2cc(Cl)ccc2-n2c(nnc2[C@H]2CC[C@H](Oc3ccccn3)CC2)C1 10.1021/acs.jmedchem.1c00863
CHEMBL5074709 212556 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate readerInhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader
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
10456892 65734 0 None 74 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
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 65734 0 None 74 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
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
162676448 182901 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 438 3 0 5 5.0 Brc1ccc2c(c1)CCCc1nnc([C@H]3CC[C@H](Oc4ccccn4)CC3)n1-2 10.1016/j.bmcl.2020.127417
CHEMBL4799412 182901 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 438 3 0 5 5.0 Brc1ccc2c(c1)CCCc1nnc([C@H]3CC[C@H](Oc4ccccn4)CC3)n1-2 10.1016/j.bmcl.2020.127417
162655262 180164 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 426 2 0 5 5.3 Cc1cc([C@H]2CC[C@H](c3nnc4n3-c3ccc(Br)cc3CCC4)CC2)no1 10.1016/j.bmcl.2020.127417
CHEMBL4756031 180164 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 426 2 0 5 5.3 Cc1cc([C@H]2CC[C@H](c3nnc4n3-c3ccc(Br)cc3CCC4)CC2)no1 10.1016/j.bmcl.2020.127417
CHEMBL5070075 212455 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate readerInhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader
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
CHEMBL5081323 212971 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate readerInhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader
ChEMBL None None None Cc1ccc2c(c1)CC(O)Cc1nnc([C@H]3CC[C@H](Oc4ccccn4)CC3)n1-2 10.1021/acs.jmedchem.1c00863
162669344 182104 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 438 2 0 3 4.1 Cc1ccccc1N1CCN(C(=O)N2CN(C(=O)C3CC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4789306 182104 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 438 2 0 3 4.1 Cc1ccccc1N1CCN(C(=O)N2CN(C(=O)C3CC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
10444 2295 9 None -61 4 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human V1A receptor expressed in HEK cells assessed as inhibition of AVP-induced intracellular calcium flux incubated for 45 mins by Indo1-AM dye based fluorescence assay relative to AVPAntagonist activity at human V1A receptor expressed in HEK cells assessed as inhibition of AVP-induced intracellular calcium flux incubated for 45 mins by Indo1-AM dye based fluorescence assay relative to AVP
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 2295 9 None -61 4 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human V1A receptor expressed in HEK cells assessed as inhibition of AVP-induced intracellular calcium flux incubated for 45 mins by Indo1-AM dye based fluorescence assay relative to AVPAntagonist activity at human V1A receptor expressed in HEK cells assessed as inhibition of AVP-induced intracellular calcium flux incubated for 45 mins by Indo1-AM dye based fluorescence assay relative to AVP
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 2295 9 None -61 4 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human V1A receptor expressed in HEK cells assessed as inhibition of AVP-induced intracellular calcium flux incubated for 45 mins by Indo1-AM dye based fluorescence assay relative to AVPAntagonist activity at human V1A receptor expressed in HEK cells assessed as inhibition of AVP-induced intracellular calcium flux incubated for 45 mins by Indo1-AM dye based fluorescence assay relative to AVP
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 2295 9 None -61 4 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human V1A receptor expressed in HEK cells assessed as inhibition of AVP-induced intracellular calcium flux incubated for 45 mins by Indo1-AM dye based fluorescence assay relative to AVPAntagonist activity at human V1A receptor expressed in HEK cells assessed as inhibition of AVP-induced intracellular calcium flux incubated for 45 mins by Indo1-AM dye based fluorescence assay relative to AVP
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
162649115 179289 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 368 2 0 5 4.8 Cc1cc([C@H]2CC[C@H](c3nnc4n3-c3ccc(Cl)cc3CC4)CC2)no1 10.1016/j.bmcl.2020.127417
CHEMBL4745524 179289 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 368 2 0 5 4.8 Cc1cc([C@H]2CC[C@H](c3nnc4n3-c3ccc(Cl)cc3CC4)CC2)no1 10.1016/j.bmcl.2020.127417
162668040 181936 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 371 1 1 4 3.3 C[C@H]1CN(C(=O)N2CCNc3cc(Cl)ccc32)CCN1c1ccccn1 10.1016/j.bmcl.2020.127416
CHEMBL4787124 181936 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 371 1 1 4 3.3 C[C@H]1CN(C(=O)N2CCNc3cc(Cl)ccc32)CCN1c1ccccn1 10.1016/j.bmcl.2020.127416
135192889 173477 0 None -25 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based assayAntagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based assay
ChEMBL 425 5 0 6 4.1 COc1ccc(-n2c(C3CC3)nnc2N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)cn1 10.1021/acsmedchemlett.9b00186
CHEMBL4543809 173477 0 None -25 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based assayAntagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based assay
ChEMBL 425 5 0 6 4.1 COc1ccc(-n2c(C3CC3)nnc2N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)cn1 10.1021/acsmedchemlett.9b00186
162658180 180479 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 466 2 0 3 4.9 Cc1ccccc1N1CCN(C(=O)N2CN(C(=O)C3CCCC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4759676 180479 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 466 2 0 3 4.9 Cc1ccccc1N1CCN(C(=O)N2CN(C(=O)C3CCCC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
162662884 181330 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 440 2 0 3 4.4 Cc1ccccc1N1CCN(C(=O)N2CN(C(=O)C(C)C)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4779447 181330 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 440 2 0 3 4.4 Cc1ccccc1N1CCN(C(=O)N2CN(C(=O)C(C)C)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
11326488 65727 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 380 2 1 6 3.3 Clc1ccc2c(c1)CNCc1nnc(C3CCN(c4ccccn4)CC3)n1-2 10.1016/j.bmcl.2011.08.038
CHEMBL1837035 65727 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 380 2 1 6 3.3 Clc1ccc2c(c1)CNCc1nnc(C3CCN(c4ccccn4)CC3)n1-2 10.1016/j.bmcl.2011.08.038
145965794 163821 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human V1A receptor expressed in HEK cells assessed as inhibition of AVP-induced intracellular calcium flux incubated for 45 mins by Indo1-AM dye based fluorescence assay relative to AVPAntagonist activity at human V1A receptor expressed in HEK cells assessed as inhibition of AVP-induced intracellular calcium flux incubated for 45 mins by Indo1-AM dye based fluorescence assay relative to AVP
ChEMBL 462 5 3 7 2.6 COC(=O)CNC(=O)NCc1ccc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)cc1C 10.1021/acs.jmedchem.8b00697
CHEMBL4212928 163821 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human V1A receptor expressed in HEK cells assessed as inhibition of AVP-induced intracellular calcium flux incubated for 45 mins by Indo1-AM dye based fluorescence assay relative to AVPAntagonist activity at human V1A receptor expressed in HEK cells assessed as inhibition of AVP-induced intracellular calcium flux incubated for 45 mins by Indo1-AM dye based fluorescence assay relative to AVP
ChEMBL 462 5 3 7 2.6 COC(=O)CNC(=O)NCc1ccc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)cc1C 10.1021/acs.jmedchem.8b00697
137212772 137413 0 None 3 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human vasopressin 1a receptor expressed in HEK293 cells assessed as inhibition of vasopressin induced IP1 accumulation pretreated for 30 mins measured 1 hr post Ab-Cryptate and IP1-d2 addition by HTRF assayAntagonist activity at human vasopressin 1a receptor expressed in HEK293 cells assessed as inhibition of vasopressin induced IP1 accumulation pretreated for 30 mins measured 1 hr post Ab-Cryptate and IP1-d2 addition by HTRF assay
ChEMBL 609 7 2 8 4.7 COc1cc(CN2CCN(C(=O)NCc3ccc(C(=O)N4Cc5cnn(C)c5Nc5ccccc54)cc3C)CC2)cc(OC)c1 10.1016/j.ejmech.2015.11.050
CHEMBL3763951 137413 0 None 3 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human vasopressin 1a receptor expressed in HEK293 cells assessed as inhibition of vasopressin induced IP1 accumulation pretreated for 30 mins measured 1 hr post Ab-Cryptate and IP1-d2 addition by HTRF assayAntagonist activity at human vasopressin 1a receptor expressed in HEK293 cells assessed as inhibition of vasopressin induced IP1 accumulation pretreated for 30 mins measured 1 hr post Ab-Cryptate and IP1-d2 addition by HTRF assay
ChEMBL 609 7 2 8 4.7 COc1cc(CN2CCN(C(=O)NCc3ccc(C(=O)N4Cc5cnn(C)c5Nc5ccccc54)cc3C)CC2)cc(OC)c1 10.1016/j.ejmech.2015.11.050
137212772 137413 0 None 3 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of vasopressin-induced IP1 accumulation preincubated for 30 mins followed by vasopressin addition measured after 1 hr by HTRF assayAntagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of vasopressin-induced IP1 accumulation preincubated for 30 mins followed by vasopressin addition measured after 1 hr by HTRF assay
ChEMBL 609 7 2 8 4.7 COc1cc(CN2CCN(C(=O)NCc3ccc(C(=O)N4Cc5cnn(C)c5Nc5ccccc54)cc3C)CC2)cc(OC)c1 10.1016/j.ejmech.2017.10.059
CHEMBL3763951 137413 0 None 3 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of vasopressin-induced IP1 accumulation preincubated for 30 mins followed by vasopressin addition measured after 1 hr by HTRF assayAntagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of vasopressin-induced IP1 accumulation preincubated for 30 mins followed by vasopressin addition measured after 1 hr by HTRF assay
ChEMBL 609 7 2 8 4.7 COc1cc(CN2CCN(C(=O)NCc3ccc(C(=O)N4Cc5cnn(C)c5Nc5ccccc54)cc3C)CC2)cc(OC)c1 10.1016/j.ejmech.2017.10.059
23598597 93663 0 None -91 2 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium levelAntagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
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 93663 0 None -91 2 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium levelAntagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
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
10359487 65710 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 333 4 0 5 3.4 Cc1nnc(C2CCN(c3ccccn3)CC2)n1Cc1ccccc1 10.1016/j.bmcl.2011.08.038
CHEMBL1837018 65710 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 333 4 0 5 3.4 Cc1nnc(C2CCN(c3ccccn3)CC2)n1Cc1ccccc1 10.1016/j.bmcl.2011.08.038
162661138 180927 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 345 2 0 5 3.5 c1ccc(N2CCC(c3nnc4n3-c3ccccc3CCC4)CC2)nc1 10.1016/j.bmcl.2020.127417
CHEMBL4764976 180927 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 345 2 0 5 3.5 c1ccc(N2CCC(c3nnc4n3-c3ccccc3CCC4)CC2)nc1 10.1016/j.bmcl.2020.127417
9829108 5165 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Evaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptorEvaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptor
ChEMBL 554 7 2 4 5.1 CN(C)CCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL106293 5165 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Evaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptorEvaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptor
ChEMBL 554 7 2 4 5.1 CN(C)CCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
2200 3259 41 None 1548 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
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 10.1016/j.bmcl.2011.08.038
3482 3259 41 None 1548 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
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 10.1016/j.bmcl.2011.08.038
60943 3259 41 None 1548 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
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 10.1016/j.bmcl.2011.08.038
CHEMBL419667 3259 41 None 1548 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
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 10.1016/j.bmcl.2011.08.038
DB13929 3259 41 None 1548 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
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 10.1016/j.bmcl.2011.08.038
162648487 179383 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 423 2 0 5 4.3 Brc1ccc2c(c1)CCCc1nnc(C3CCN(c4ccccn4)CC3)n1-2 10.1016/j.bmcl.2020.127417
CHEMBL4746716 179383 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 423 2 0 5 4.3 Brc1ccc2c(c1)CCCc1nnc(C3CCN(c4ccccn4)CC3)n1-2 10.1016/j.bmcl.2020.127417
23598619 94103 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium levelAntagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
ChEMBL 498 4 1 4 5.6 COC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
CHEMBL251771 94103 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium levelAntagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
ChEMBL 498 4 1 4 5.6 COC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
11337030 65704 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 349 4 0 6 3.4 COc1ccc(-n2c(C)nnc2C2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmcl.2011.08.038
CHEMBL1837012 65704 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 349 4 0 6 3.4 COc1ccc(-n2c(C)nnc2C2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmcl.2011.08.038
21064040 65722 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 377 3 0 7 3.1 COc1ccc2c(c1)COCc1nnc(C3CCN(c4ccccn4)CC3)n1-2 10.1016/j.bmcl.2011.08.038
CHEMBL1837030 65722 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 377 3 0 7 3.1 COc1ccc2c(c1)COCc1nnc(C3CCN(c4ccccn4)CC3)n1-2 10.1016/j.bmcl.2011.08.038
162661774 180823 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 439 3 0 3 4.1 Cc1ccccc1N1CCN(C(=O)C2CN(C(=O)C(C)C)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4763639 180823 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 439 3 0 3 4.1 Cc1ccccc1N1CCN(C(=O)C2CN(C(=O)C(C)C)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
44336418 107701 0 None 2 2 Human 6.9 pIC50 = 6.9 Functional
Evaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptorEvaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a 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 107701 0 None 2 2 Human 6.9 pIC50 = 6.9 Functional
Evaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptorEvaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a 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
145961670 160817 0 None 123 4 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human liver vasopressin V1a receptor expressed in CHO cells assessed as inhibition of agonist-induced intracellular calcium flux preincubated for 20 mins followed by AVP addition measured for 5 mins by Fluo-4-AM dye based FLIPR assayAntagonist activity at human liver vasopressin V1a receptor expressed in CHO cells assessed as inhibition of agonist-induced intracellular calcium flux preincubated for 20 mins followed by AVP addition 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 160817 0 None 123 4 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human liver vasopressin V1a receptor expressed in CHO cells assessed as inhibition of agonist-induced intracellular calcium flux preincubated for 20 mins followed by AVP addition measured for 5 mins by Fluo-4-AM dye based FLIPR assayAntagonist activity at human liver vasopressin V1a receptor expressed in CHO cells assessed as inhibition of agonist-induced intracellular calcium flux preincubated for 20 mins followed by AVP addition 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
162646538 179026 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 412 1 0 3 3.8 CC(=O)N1CCN(C(=O)N2CCN(c3ccccc3C)CC2)c2ccc(Cl)cc21 10.1016/j.bmcl.2020.127416
CHEMBL4742335 179026 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 412 1 0 3 3.8 CC(=O)N1CCN(C(=O)N2CCN(c3ccccc3C)CC2)c2ccc(Cl)cc21 10.1016/j.bmcl.2020.127416
162656367 180308 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 370 1 1 3 3.8 Cc1ccccc1N1CCN(C(=O)N2CCNc3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4757593 180308 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 370 1 1 3 3.8 Cc1ccccc1N1CCN(C(=O)N2CCNc3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2020.127416
162660975 181275 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 365 2 0 5 3.8 Clc1ccc2c(c1)CCc1nnc(C3CCN(c4ccccn4)CC3)n1-2 10.1016/j.bmcl.2020.127417
CHEMBL4778700 181275 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 365 2 0 5 3.8 Clc1ccc2c(c1)CCc1nnc(C3CCN(c4ccccn4)CC3)n1-2 10.1016/j.bmcl.2020.127417
56672569 65713 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 347 4 0 5 3.7 Cc1ccc(Cn2c(C)nnc2C2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmcl.2011.08.038
CHEMBL1837021 65713 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 347 4 0 5 3.7 Cc1ccc(Cn2c(C)nnc2C2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmcl.2011.08.038
44352783 116281 0 None -4 2 Human 6.8 pIC50 = 6.8 Functional
Inhibition of vasopressin induced calcium immobilization in human V1a receptor expressing cellsInhibition of vasopressin induced calcium immobilization in human V1a 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 116281 0 None -4 2 Human 6.8 pIC50 = 6.8 Functional
Inhibition of vasopressin induced calcium immobilization in human V1a receptor expressing cellsInhibition of vasopressin induced calcium immobilization in human V1a 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
44336403 5310 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Evaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptorEvaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptor
ChEMBL 580 7 2 4 5.6 O=C(NCCN1CCCC1)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL107058 5310 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Evaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptorEvaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptor
ChEMBL 580 7 2 4 5.6 O=C(NCCN1CCCC1)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
3537 3941 14 None -57 4 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at V1A receptor (unknown origin) by cAMP accumulation assayAntagonist activity at V1A 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 3941 14 None -57 4 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at V1A receptor (unknown origin) by cAMP accumulation assayAntagonist activity at V1A 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 3941 14 None -57 4 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at V1A receptor (unknown origin) by cAMP accumulation assayAntagonist activity at V1A 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
11740204 65714 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 375 7 0 5 4.4 CCCCc1nnc(C2CCN(c3ccccn3)CC2)n1Cc1ccccc1 10.1016/j.bmcl.2011.08.038
CHEMBL1837022 65714 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 375 7 0 5 4.4 CCCCc1nnc(C2CCN(c3ccccn3)CC2)n1Cc1ccccc1 10.1016/j.bmcl.2011.08.038
21925639 65723 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 381 2 0 6 3.7 Clc1ccc2c(c1)COCc1nnc(C3CCN(c4ccccn4)CC3)n1-2 10.1016/j.bmcl.2011.08.038
CHEMBL1837031 65723 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 381 2 0 6 3.7 Clc1ccc2c(c1)COCc1nnc(C3CCN(c4ccccn4)CC3)n1-2 10.1016/j.bmcl.2011.08.038
162647212 179121 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 391 1 1 4 3.6 O=C(N1CCN(c2ncccc2Cl)CC1)N1CCNc2cc(Cl)ccc21 10.1016/j.bmcl.2020.127416
CHEMBL4743785 179121 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 391 1 1 4 3.6 O=C(N1CCN(c2ncccc2Cl)CC1)N1CCNc2cc(Cl)ccc21 10.1016/j.bmcl.2020.127416
135192932 170962 0 None -190 4 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based assayAntagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based 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 170962 0 None -190 4 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based assayAntagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based 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
9828129 116121 0 None -91 2 Human 5.8 pIC50 = 5.8 Functional
Inhibition of vasopressin induced calcium immobilization in human V1a receptor expressing cellsInhibition of vasopressin induced calcium immobilization in human V1a 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 116121 0 None -91 2 Human 5.8 pIC50 = 5.8 Functional
Inhibition of vasopressin induced calcium immobilization in human V1a receptor expressing cellsInhibition of vasopressin induced calcium immobilization in human V1a 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
10318802 65719 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 400 6 0 8 2.7 c1ccc(Cn2c(Cn3nccn3)nnc2C2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmcl.2011.08.038
CHEMBL1837027 65719 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 400 6 0 8 2.7 c1ccc(Cn2c(Cn3nccn3)nnc2C2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmcl.2011.08.038
162646888 178979 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 437 3 0 3 3.8 Cc1ccccc1N1CCN(C(=O)C2CN(C(=O)C3CC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4741743 178979 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 437 3 0 3 3.8 Cc1ccccc1N1CCN(C(=O)C2CN(C(=O)C3CC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
142391805 173405 0 None -35 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based assayAntagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based assay
ChEMBL 435 5 0 6 4.2 COc1ccc(-n2c(C(F)F)nnc2N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)cn1 10.1021/acsmedchemlett.9b00186
CHEMBL4541860 173405 0 None -35 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based assayAntagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based assay
ChEMBL 435 5 0 6 4.2 COc1ccc(-n2c(C(F)F)nnc2N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)cn1 10.1021/acsmedchemlett.9b00186
145976595 163163 0 None -2 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human V1A receptor expressed in human HeLa cells assessed as inhibition of AVP-induced cAMP accumulation incubated for 10 mins by radioimmunoassayAntagonist activity at human V1A 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 163163 0 None -2 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human V1A receptor expressed in human HeLa cells assessed as inhibition of AVP-induced cAMP accumulation incubated for 10 mins by radioimmunoassayAntagonist activity at human V1A 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
44444761 93731 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium levelAntagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
ChEMBL 532 4 1 4 6.2 COC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3Cl)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
CHEMBL249536 93731 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium levelAntagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
ChEMBL 532 4 1 4 6.2 COC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3Cl)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
135192895 173414 0 None -8 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based assayAntagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based 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
CHEMBL4542267 173414 0 None -8 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based assayAntagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based 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
11473073 65705 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 333 3 0 5 3.7 Cc1ccccc1-n1c(C)nnc1C1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2011.08.038
CHEMBL1837013 65705 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 333 3 0 5 3.7 Cc1ccccc1-n1c(C)nnc1C1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2011.08.038
59657596 118161 25 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 437 4 0 4 4.5 CN(C)CCn1cc(C(=O)N2CCC3(CC2)OCc2ccccc23)c2ccc(Cl)cc21 10.1016/j.bmcl.2020.127416
CHEMBL3416885 118161 25 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 437 4 0 4 4.5 CN(C)CCn1cc(C(=O)N2CCC3(CC2)OCc2ccccc23)c2ccc(Cl)cc21 10.1016/j.bmcl.2020.127416
59657596 118161 25 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate readerInhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader
ChEMBL 437 4 0 4 4.5 CN(C)CCn1cc(C(=O)N2CCC3(CC2)OCc2ccccc23)c2ccc(Cl)cc21 10.1021/acs.jmedchem.1c00863
CHEMBL3416885 118161 25 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate readerInhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader
ChEMBL 437 4 0 4 4.5 CN(C)CCn1cc(C(=O)N2CCC3(CC2)OCc2ccccc23)c2ccc(Cl)cc21 10.1021/acs.jmedchem.1c00863
162655215 180227 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 382 2 0 5 5.1 Cc1cc([C@H]2CC[C@H](c3nnc4n3-c3ccc(Cl)cc3CCC4)CC2)no1 10.1016/j.bmcl.2020.127417
CHEMBL4756737 180227 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 382 2 0 5 5.1 Cc1cc([C@H]2CC[C@H](c3nnc4n3-c3ccc(Cl)cc3CCC4)CC2)no1 10.1016/j.bmcl.2020.127417
162655954 180185 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 465 3 0 3 5.3 Cc1ccccc1N1CCN(C(=O)N2C[C@@H](C(=O)C3CCCC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4756212 180185 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 465 3 0 3 5.3 Cc1ccccc1N1CCN(C(=O)N2C[C@@H](C(=O)C3CCCC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
162643927 181225 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 466 2 0 3 4.2 Cc1ccccc1N1CCN(C(=O)N2C[C@@H](C(=O)N3CCCC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127417
CHEMBL4778087 181225 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 466 2 0 3 4.2 Cc1ccccc1N1CCN(C(=O)N2C[C@@H](C(=O)N3CCCC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127417
162658238 180424 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 369 2 0 5 3.5 C#Cc1ccc2c(c1)CCCc1nnc(C3CCN(c4ccccn4)CC3)n1-2 10.1016/j.bmcl.2020.127417
CHEMBL4759005 180424 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 369 2 0 5 3.5 C#Cc1ccc2c(c1)CCCc1nnc(C3CCN(c4ccccn4)CC3)n1-2 10.1016/j.bmcl.2020.127417
10411308 199549 0 None -2 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at V1A receptor (unknown origin)Antagonist activity at V1A 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 199549 0 None -2 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at V1A receptor (unknown origin)Antagonist activity at V1A receptor (unknown origin)
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.8b00697
17989455 65287 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 361 2 0 6 3.4 Cc1ccc2c(c1)COCc1nnc(C3CCN(c4ccccn4)CC3)n1-2 10.1016/j.bmcl.2011.08.038
CHEMBL1834004 65287 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 361 2 0 6 3.4 Cc1ccc2c(c1)COCc1nnc(C3CCN(c4ccccn4)CC3)n1-2 10.1016/j.bmcl.2011.08.038
22017591 65715 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 377 7 0 6 3.6 CCOCc1nnc(C2CCN(c3ccccn3)CC2)n1Cc1ccccc1 10.1016/j.bmcl.2011.08.038
CHEMBL1837023 65715 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 377 7 0 6 3.6 CCOCc1nnc(C2CCN(c3ccccn3)CC2)n1Cc1ccccc1 10.1016/j.bmcl.2011.08.038
162664826 181516 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 448 2 0 4 3.1 Cc1ccccc1N1CCN(C(=O)N2CN(S(C)(=O)=O)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4781783 181516 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 448 2 0 4 3.1 Cc1ccccc1N1CCN(C(=O)N2CN(S(C)(=O)=O)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
23598595 154265 0 None 2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium levelAntagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
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 154265 0 None 2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium levelAntagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
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
162645320 178926 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 360 3 0 5 4.3 c1ccc(O[C@H]2CC[C@H](c3nnc4n3-c3ccccc3CCC4)CC2)nc1 10.1016/j.bmcl.2020.127417
CHEMBL4741178 178926 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 360 3 0 5 4.3 c1ccc(O[C@H]2CC[C@H](c3nnc4n3-c3ccccc3CCC4)CC2)nc1 10.1016/j.bmcl.2020.127417
4391207 56928 1 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 311 3 0 3 4.9 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1 10.1016/j.bmcl.2011.08.038
CHEMBL1649949 56928 1 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 311 3 0 3 4.9 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1 10.1016/j.bmcl.2011.08.038
162658540 180521 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 369 1 0 2 4.3 Cc1ccccc1N1CCN(C(=O)N2CCCc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4760164 180521 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 369 1 0 2 4.3 Cc1ccccc1N1CCN(C(=O)N2CCCc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
44352804 18770 0 None -24 2 Human 5.7 pIC50 = 5.7 Functional
Inhibition of vasopressin induced calcium immobilization in human V1a receptor expressing cellsInhibition of vasopressin induced calcium immobilization in human V1a 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 18770 0 None -24 2 Human 5.7 pIC50 = 5.7 Functional
Inhibition of vasopressin induced calcium immobilization in human V1a receptor expressing cellsInhibition of vasopressin induced calcium immobilization in human V1a 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
162648022 179394 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 479 3 0 3 5.0 Cc1ccccc1N1CCN(C(=O)C2CN(C(=O)C3CCCCC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4746818 179394 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 479 3 0 3 5.0 Cc1ccccc1N1CCN(C(=O)C2CN(C(=O)C3CCCCC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
44352757 117950 0 None -58 2 Human 5.7 pIC50 = 5.7 Functional
Inhibition of vasopressin induced calcium immobilization in human V1a receptor expressing cellsInhibition of vasopressin induced calcium immobilization in human V1a 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 117950 0 None -58 2 Human 5.7 pIC50 = 5.7 Functional
Inhibition of vasopressin induced calcium immobilization in human V1a receptor expressing cellsInhibition of vasopressin induced calcium immobilization in human V1a 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
162655687 180200 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 452 5 0 7 4.6 COC(=O)CC1Cc2cc(Cl)ccc2-n2c1nnc2[C@H]1CC[C@H](Oc2ccccn2)CC1 10.1016/j.bmcl.2020.127417
CHEMBL4756354 180200 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 452 5 0 7 4.6 COC(=O)CC1Cc2cc(Cl)ccc2-n2c1nnc2[C@H]1CC[C@H](Oc2ccccn2)CC1 10.1016/j.bmcl.2020.127417
10444 2295 9 None -61 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human V1a receptor expressed in HEK293FT cells assessed as inhibition of AVP-induced response incubated for 30 mins by beta-arrestin recruitment assayAntagonist activity at human V1a receptor expressed in HEK293FT cells assessed as inhibition of AVP-induced response 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 2295 9 None -61 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human V1a receptor expressed in HEK293FT cells assessed as inhibition of AVP-induced response incubated for 30 mins by beta-arrestin recruitment assayAntagonist activity at human V1a receptor expressed in HEK293FT cells assessed as inhibition of AVP-induced response 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 2295 9 None -61 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human V1a receptor expressed in HEK293FT cells assessed as inhibition of AVP-induced response incubated for 30 mins by beta-arrestin recruitment assayAntagonist activity at human V1a receptor expressed in HEK293FT cells assessed as inhibition of AVP-induced response 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 2295 9 None -61 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human V1a receptor expressed in HEK293FT cells assessed as inhibition of AVP-induced response incubated for 30 mins by beta-arrestin recruitment assayAntagonist activity at human V1a receptor expressed in HEK293FT cells assessed as inhibition of AVP-induced response 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
44336799 106747 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Evaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptorEvaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptor
ChEMBL 596 7 2 5 4.8 O=C(NCCN1CCOCC1)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL316736 106747 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Evaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptorEvaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptor
ChEMBL 596 7 2 5 4.8 O=C(NCCN1CCOCC1)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
56672567 65707 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 344 3 0 6 3.2 Cc1nnc(C2CCN(c3ccccn3)CC2)n1-c1ccc(C#N)cc1 10.1016/j.bmcl.2011.08.038
CHEMBL1837015 65707 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 344 3 0 6 3.2 Cc1nnc(C2CCN(c3ccccn3)CC2)n1-c1ccc(C#N)cc1 10.1016/j.bmcl.2011.08.038
22017582 65718 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 407 8 1 7 2.7 O=C(O)COCc1nnc(C2CCN(c3ccccn3)CC2)n1Cc1ccccc1 10.1016/j.bmcl.2011.08.038
CHEMBL1837026 65718 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 407 8 1 7 2.7 O=C(O)COCc1nnc(C2CCN(c3ccccn3)CC2)n1Cc1ccccc1 10.1016/j.bmcl.2011.08.038
22017577 65716 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 418 6 0 7 2.9 c1ccc(Cn2c(CN3CCOCC3)nnc2C2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmcl.2011.08.038
CHEMBL1837024 65716 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 418 6 0 7 2.9 c1ccc(Cn2c(CN3CCOCC3)nnc2C2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmcl.2011.08.038
162670181 182171 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 465 3 0 3 5.3 Cc1ccccc1N1CCN(C(=O)N2C[C@H](C(=O)C3CCCC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4790089 182171 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 465 3 0 3 5.3 Cc1ccccc1N1CCN(C(=O)N2C[C@H](C(=O)C3CCCC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
162667087 181857 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 348 2 0 5 4.5 Cc1cc([C@H]2CC[C@H](c3nnc4n3-c3ccccc3CCC4)CC2)no1 10.1016/j.bmcl.2020.127417
CHEMBL4786172 181857 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 348 2 0 5 4.5 Cc1cc([C@H]2CC[C@H](c3nnc4n3-c3ccccc3CCC4)CC2)no1 10.1016/j.bmcl.2020.127417
162676230 182743 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 373 3 0 5 4.1 CCc1ccc2c(c1)CCCc1nnc(C3CCN(c4ccccn4)CC3)n1-2 10.1016/j.bmcl.2020.127417
CHEMBL4797387 182743 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 373 3 0 5 4.1 CCc1ccc2c(c1)CCCc1nnc(C3CCN(c4ccccn4)CC3)n1-2 10.1016/j.bmcl.2020.127417
162657843 180563 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 370 2 0 4 3.4 CN1CCN(C(=O)C2CCN(c3ccccn3)CC2)c2ccc(Cl)cc21 10.1016/j.bmcl.2020.127416
CHEMBL4760698 180563 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 370 2 0 4 3.4 CN1CCN(C(=O)C2CCN(c3ccccn3)CC2)c2ccc(Cl)cc21 10.1016/j.bmcl.2020.127416
162652318 179742 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 356 2 1 4 3.4 O=C(C1CCN(c2ccccn2)CC1)N1CCNc2cc(Cl)ccc21 10.1016/j.bmcl.2020.127417
CHEMBL4751140 179742 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 356 2 1 4 3.4 O=C(C1CCN(c2ccccn2)CC1)N1CCNc2cc(Cl)ccc21 10.1016/j.bmcl.2020.127417
25133000 93760 0 None -2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium levelAntagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
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 93760 0 None -2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium levelAntagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
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
21925586 65728 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 360 2 0 6 3.0 CN1Cc2ccccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
CHEMBL1837036 65728 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 360 2 0 6 3.0 CN1Cc2ccccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
162648022 179394 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 479 3 0 3 5.0 Cc1ccccc1N1CCN(C(=O)C2CN(C(=O)C3CCCCC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4746818 179394 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 479 3 0 3 5.0 Cc1ccccc1N1CCN(C(=O)C2CN(C(=O)C3CCCCC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
162665294 181791 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 383 0 1 3 4.2 O=C(N1CCC2(CC1)OCc1ccccc12)N1CCNc2cc(Cl)ccc21 10.1016/j.bmcl.2020.127416
CHEMBL4785083 181791 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 383 0 1 3 4.2 O=C(N1CCC2(CC1)OCc1ccccc12)N1CCNc2cc(Cl)ccc21 10.1016/j.bmcl.2020.127416
162661801 180873 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 336 1 1 3 3.2 Cc1ccccc1N1CCN(C(=O)N2CCNc3ccccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4764410 180873 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 336 1 1 3 3.2 Cc1ccccc1N1CCN(C(=O)N2CCNc3ccccc32)CC1 10.1016/j.bmcl.2020.127416
135192983 175544 8 None -190 4 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based assayAntagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based 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 175544 8 None -190 4 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based assayAntagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based 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
10474163 65712 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 367 4 0 5 4.1 Cc1nnc(C2CCN(c3ccccn3)CC2)n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2011.08.038
CHEMBL1837020 65712 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 367 4 0 5 4.1 Cc1nnc(C2CCN(c3ccccn3)CC2)n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2011.08.038
23598600 5295 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
Evaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptorEvaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a 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 5295 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
Evaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptorEvaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a 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
44336784 108721 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
Evaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptorEvaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a 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 108721 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
Evaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptorEvaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a 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
56682562 65720 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 434 6 0 8 3.4 Clc1cccc(Cn2c(Cn3nccn3)nnc2C2CCN(c3ccccn3)CC2)c1 10.1016/j.bmcl.2011.08.038
CHEMBL1837028 65720 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 434 6 0 8 3.4 Clc1cccc(Cn2c(Cn3nccn3)nnc2C2CCN(c3ccccn3)CC2)c1 10.1016/j.bmcl.2011.08.038
10615 566 26 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1016/j.bmcl.2020.127416
46200932 566 26 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1016/j.bmcl.2020.127416
CHEMBL4297183 566 26 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1016/j.bmcl.2020.127416
DB14823 566 26 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1016/j.bmcl.2020.127416
151171 1141 43 None 3 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human Vasopressin V1a receptor assessed as inhibition of intracellular calcium mobilization by FLIPR assayAntagonist activity at human Vasopressin V1a receptor assessed as inhibition of intracellular calcium mobilization by FLIPR assay
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 1141 43 None 3 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human Vasopressin V1a receptor assessed as inhibition of intracellular calcium mobilization by FLIPR assayAntagonist activity at human Vasopressin V1a receptor assessed as inhibition of intracellular calcium mobilization by FLIPR assay
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 1141 43 None 3 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human Vasopressin V1a receptor assessed as inhibition of intracellular calcium mobilization by FLIPR assayAntagonist activity at human Vasopressin V1a receptor assessed as inhibition of intracellular calcium mobilization by FLIPR assay
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 1141 43 None 3 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human Vasopressin V1a receptor assessed as inhibition of intracellular calcium mobilization by FLIPR assayAntagonist activity at human Vasopressin V1a receptor assessed as inhibition of intracellular calcium mobilization by FLIPR assay
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 1141 43 None 3 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human Vasopressin V1a receptor assessed as inhibition of intracellular calcium mobilization by FLIPR assayAntagonist activity at human Vasopressin V1a receptor assessed as inhibition of intracellular calcium mobilization by FLIPR assay
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 1141 43 None 3 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human Vasopressin V1a receptor assessed as inhibition of intracellular calcium mobilization by FLIPR assayAntagonist activity at human Vasopressin V1a receptor assessed as inhibition of intracellular calcium mobilization by FLIPR assay
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
10615 566 26 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate readerInhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader
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 566 26 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate readerInhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader
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 566 26 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate readerInhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader
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 566 26 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate readerInhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1021/acs.jmedchem.1c00863
10615 566 26 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1016/j.bmcl.2020.127417
46200932 566 26 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1016/j.bmcl.2020.127417
CHEMBL4297183 566 26 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1016/j.bmcl.2020.127417
DB14823 566 26 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1016/j.bmcl.2020.127417
56672570 65730 0 None 9 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
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 65730 0 None 9 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 438 2 0 7 3.8 COC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
162660856 181287 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 379 2 0 5 4.2 Clc1ccc2c(c1)CCCc1nnc(C3CCN(c4ccccn4)CC3)n1-2 10.1016/j.bmcl.2020.127417
CHEMBL4778839 181287 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayInhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 379 2 0 5 4.2 Clc1ccc2c(c1)CCCc1nnc(C3CCN(c4ccccn4)CC3)n1-2 10.1016/j.bmcl.2020.127417
162672471 182459 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 384 1 0 3 3.8 Cc1ccccc1N1CCN(C(=O)N2CCN(C)c3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4794001 182459 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 384 1 0 3 3.8 Cc1ccccc1N1CCN(C(=O)N2CCN(C)c3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
11237434 65729 7 None 102 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate readerInhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader
ChEMBL 394 2 0 6 3.6 CN1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1021/acs.jmedchem.1c00863
CHEMBL1837037 65729 7 None 102 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate readerInhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader
ChEMBL 394 2 0 6 3.6 CN1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1021/acs.jmedchem.1c00863
25132999 154364 0 None 3 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium levelAntagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
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 154364 0 None 3 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium levelAntagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
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
11278622 65703 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 319 3 0 5 3.4 Cc1nnc(C2CCN(c3ccccn3)CC2)n1-c1ccccc1 10.1016/j.bmcl.2011.08.038
CHEMBL1837011 65703 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 319 3 0 5 3.4 Cc1nnc(C2CCN(c3ccccn3)CC2)n1-c1ccccc1 10.1016/j.bmcl.2011.08.038
21925546 65721 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 347 2 0 6 3.1 c1ccc(N2CCC(c3nnc4n3-c3ccccc3COC4)CC2)nc1 10.1016/j.bmcl.2011.08.038
CHEMBL1837029 65721 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 347 2 0 6 3.1 c1ccc(N2CCC(c3nnc4n3-c3ccccc3COC4)CC2)nc1 10.1016/j.bmcl.2011.08.038
162647523 179197 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 428 2 1 4 2.7 Cc1ccccc1N1CCN(C(=O)N2CN(C(=O)CO)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4744606 179197 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 428 2 1 4 2.7 Cc1ccccc1N1CCN(C(=O)N2CN(C(=O)CO)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
162653495 179912 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 465 3 0 3 4.6 Cc1ccccc1N1CCN(C(=O)C2CN(C(=O)C3CCCC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4753130 179912 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 465 3 0 3 4.6 Cc1ccccc1N1CCN(C(=O)C2CN(C(=O)C3CCCC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
162656299 180369 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 474 2 0 3 5.0 Cc1ccccc1N1CCN(C(=O)N2CN(C(=O)c3ccccc3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4758331 180369 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 474 2 0 3 5.0 Cc1ccccc1N1CCN(C(=O)N2CN(C(=O)c3ccccc3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
145963213 160934 0 None 8 4 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human liver vasopressin V1a receptor expressed in CHO cells assessed as inhibition of agonist-induced intracellular calcium flux preincubated for 20 mins followed by AVP addition measured for 5 mins by Fluo-4-AM dye based FLIPR assayAntagonist activity at human liver vasopressin V1a receptor expressed in CHO cells assessed as inhibition of agonist-induced intracellular calcium flux preincubated for 20 mins followed by AVP addition 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 160934 0 None 8 4 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human liver vasopressin V1a receptor expressed in CHO cells assessed as inhibition of agonist-induced intracellular calcium flux preincubated for 20 mins followed by AVP addition measured for 5 mins by Fluo-4-AM dye based FLIPR assayAntagonist activity at human liver vasopressin V1a receptor expressed in CHO cells assessed as inhibition of agonist-induced intracellular calcium flux preincubated for 20 mins followed by AVP addition 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
54586172 61582 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium releaseAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release
ChEMBL 485 7 3 3 4.2 O=C(N[C@@H]1C[C@@H]2CC[C@H](C1)N2)[C@@H](Cc1ccc(Cl)cc1)NC(=O)C1(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2011.02.096
CHEMBL1774024 61582 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium releaseAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release
ChEMBL 485 7 3 3 4.2 O=C(N[C@@H]1C[C@@H]2CC[C@H](C1)N2)[C@@H](Cc1ccc(Cl)cc1)NC(=O)C1(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2011.02.096
11157078 93761 5 None 2 4 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium levelAntagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
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 93761 5 None 2 4 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium levelAntagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
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
162643184 181096 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 369 1 1 2 4.9 Cc1ccccc1C1CCN(C(=O)N2CCNc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4776471 181096 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 369 1 1 2 4.9 Cc1ccccc1C1CCN(C(=O)N2CCNc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
11432362 93703 0 None 1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium levelAntagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
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 93703 0 None 1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium levelAntagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
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
135192928 174332 0 None -125 4 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based assayAntagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based 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 174332 0 None -125 4 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based assayAntagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based 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
162651435 179625 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 383 1 0 2 4.7 Cc1ccccc1N1CCN(C(=O)N2CCCCc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4749660 179625 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 383 1 0 2 4.7 Cc1ccccc1N1CCN(C(=O)N2CCCCc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL5085869 213223 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate readerInhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader
ChEMBL None None None Cc1ccc2c(c1)-n1c(nnc1[C@H]1CC[C@H](Oc3ccccn3)CC1)CC(O)C2 10.1021/acs.jmedchem.1c00863
10461417 106817 0 None 7 2 Human 8.4 pIC50 = 8.4 Functional
Evaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptorEvaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a 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 106817 0 None 7 2 Human 8.4 pIC50 = 8.4 Functional
Evaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptorEvaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a 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
44336379 106933 0 None 6 2 Human 8.4 pIC50 = 8.4 Functional
Evaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptorEvaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a 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 106933 0 None 6 2 Human 8.4 pIC50 = 8.4 Functional
Evaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptorEvaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a 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
10345610 65733 0 None 204 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
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 65733 0 None 204 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assayAntagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
ChEMBL 422 2 0 6 3.6 CC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
162648022 179394 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 479 3 0 3 5.0 Cc1ccccc1N1CCN(C(=O)C2CN(C(=O)C3CCCCC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4746818 179394 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 479 3 0 3 5.0 Cc1ccccc1N1CCN(C(=O)C2CN(C(=O)C3CCCCC3)Cc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
162658817 180409 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 370 1 1 3 3.5 Cc1ccccc1N1CCN(C(=O)N2CNCc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
CHEMBL4758799 180409 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 370 1 1 3 3.5 Cc1ccccc1N1CCN(C(=O)N2CNCc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2020.127416
162671049 182238 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 703 11 1 6 5.6 C[C@H](NC(=O)[C@@H](CC(=O)N1CCC(N2CCCCC2)CC1)N1C(=O)[C@@H](N2C(=O)OC[C@@H]2c2ccccc2)[C@H]1/C=C/c1ccccc1)c1ccccc1 10.1016/j.bmcl.2020.127416
CHEMBL4790970 182238 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assayAntagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
ChEMBL 703 11 1 6 5.6 C[C@H](NC(=O)[C@@H](CC(=O)N1CCC(N2CCCCC2)CC1)N1C(=O)[C@@H](N2C(=O)OC[C@@H]2c2ccccc2)[C@H]1/C=C/c1ccccc1)c1ccccc1 10.1016/j.bmcl.2020.127416
46890707 6649 0 None 20 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human Vasopressin V1a receptor assessed as inhibition of intracellular calcium mobilization by FLIPR assayAntagonist activity at human Vasopressin V1a receptor assessed as inhibition of intracellular calcium mobilization by FLIPR assay
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 6649 0 None 20 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human Vasopressin V1a receptor assessed as inhibition of intracellular calcium mobilization by FLIPR assayAntagonist activity at human Vasopressin V1a receptor assessed as inhibition of intracellular calcium mobilization by FLIPR assay
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