Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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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 3901 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 3901 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 3901 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 3901 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 3901 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 3901 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 3901 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 3901 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 3901 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 3901 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 207260 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 207260 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 207234 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 207234 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 207263 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 207263 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 207232 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 114471 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 114471 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 161801 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 161801 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 207232 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 207261 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 207261 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 207260 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 207260 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 114472 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 114472 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 162293 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 162293 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 207235 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 207235 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 2923 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 2923 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 2923 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 2923 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 2923 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 2923 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 207234 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 207234 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 207262 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 3901 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 3901 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 3901 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 3901 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 3901 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 207262 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 3901 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 3901 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 3901 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 3901 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 3901 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 207275 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 207275 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 207233 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 207233 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 207263 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 207263 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 207233 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 207233 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 207247 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 207247 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 207230 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 207230 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 207259 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 207259 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 207232 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 207232 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 207264 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 207264 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 207269 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 64432 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 64432 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 207269 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 64432 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 64432 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 3508 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 3508 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 3508 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 3508 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 3508 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 3508 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 3508 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 3508 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 207235 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 207235 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 207270 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 207270 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 207242 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 207242 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 207247 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 207259 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 207247 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 207259 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 207274 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 207274 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 207236 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 207236 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 207230 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 207230 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 207276 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 207276 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 207240 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 207240 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 64278 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 64278 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 64457 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 64457 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 64457 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 64457 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 207238 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 207229 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 207238 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 207256 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 207256 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 207229 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 207241 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 207241 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 207258 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 207258 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 64278 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 64278 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 64278 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 64278 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 207237 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 207243 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 207255 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 207272 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 178694 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 178694 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 207255 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 207272 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 207248 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 64275 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 64275 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 54739 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 54739 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 54739 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 64275 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 64275 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 207248 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 207253 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 207253 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 207273 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 98110 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 98110 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 29973 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 29973 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 207273 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 207249 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 207245 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 207249 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 207245 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 207246 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 207244 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 207246 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 207244 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 55787 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 55787 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 55787 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 64282 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 64282 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 64282 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 64282 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 35160 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 35160 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 35160 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 207228 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 207228 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 207268 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 107087 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 107087 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 207268 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 207237 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 64281 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 64281 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 207275 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 64281 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 64281 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 207275 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 207271 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 207271 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 3508 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 3508 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 3508 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 3508 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 207239 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 3508 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 3508 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 3508 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 3508 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 207239 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 207242 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 207242 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 64287 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 64287 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 64287 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 64287 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 64281 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 64281 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 64281 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 64281 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 207237 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 207237 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 64456 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 64456 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 55679 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 55679 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 55679 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 64456 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 64456 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 54970 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 54970 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 54970 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 48568 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 48568 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 2923 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 2923 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 2923 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 2923 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 2923 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 2923 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 207231 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 207266 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 207257 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 207257 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 64276 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 64276 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 64276 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 64276 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 64286 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 64286 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 64286 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 64286 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 207231 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 207266 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 64455 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 64455 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 64455 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 64455 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 64279 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 64279 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 64279 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 64279 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 207274 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 207274 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 64285 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 64285 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 64287 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 64287 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 64285 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 64285 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 64287 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 64287 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 168398 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 168398 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 39891 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 39891 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 41432 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 41432 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 64284 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 64284 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 64284 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 64284 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 64277 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 64277 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 64277 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 64277 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 207265 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 207265 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 207256 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 207256 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 64454 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 64454 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 64454 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 64454 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 51462 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 51462 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 24198 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 24198 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 64274 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 64274 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 64274 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 64274 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 207250 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 207250 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 207251 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 207251 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 207254 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 2923 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 2923 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 2923 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 2923 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 2923 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 2923 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 207254 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 207252 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 64280 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 64280 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 207252 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 207240 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 64280 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 64280 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 207240 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 207229 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 207229 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 72557 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 72557 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 2923 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 2923 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 2923 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 2923 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 2923 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 2923 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 65716 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 65716 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 182920 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 182920 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 182920 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 182920 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 212448 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 212546 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 65719 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 65719 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 182891 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 182891 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 180154 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 180154 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 212445 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 212961 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 182094 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 182094 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 2285 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 2285 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 2285 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 2285 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 179279 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 179279 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 181926 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 181926 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 173467 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 173467 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 180469 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 180469 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 181320 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 181320 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 65712 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 65712 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 163810 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 163810 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 137400 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 137400 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 137400 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 137400 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 93650 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 93650 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 65695 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 65695 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 180917 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 180917 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 5150 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 5150 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 3247 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 3247 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 3247 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 3247 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 3247 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 179373 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 179373 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 94090 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 94090 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 65689 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 65689 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 65707 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 65707 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 180813 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 180813 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 107688 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 107688 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 160805 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 160805 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 179016 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 179016 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 180298 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 180298 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 181265 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 181265 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 65698 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 65698 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 116268 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 116268 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 5295 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 5295 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 3929 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 3929 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 3929 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 65699 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 65699 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 65708 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 65708 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 179111 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 179111 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 170952 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 170952 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 116108 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 116108 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 65704 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 65704 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 178969 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 178969 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 173395 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 173395 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 163152 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 163152 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 93718 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 93718 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 173404 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 173404 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 65690 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 65690 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 118148 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 118148 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 118148 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 118148 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 180217 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 180217 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 180175 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 180175 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 181215 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 181215 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 180414 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 180414 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 199539 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 199539 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 65272 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 65272 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 65700 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 65700 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 181506 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 181506 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 154253 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 154253 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 178916 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 178916 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 56913 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 56913 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 180511 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 180511 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 18755 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 18755 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 179384 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 179384 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 117937 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 117937 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 180190 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 180190 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 2285 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 2285 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 2285 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 2285 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 106734 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 106734 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 65692 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 65692 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 65703 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 65703 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 65701 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 65701 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 182161 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 182161 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 181847 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 181847 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 182733 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 182733 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 180553 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 180553 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 179732 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 179732 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 93747 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 93747 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 65713 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 65713 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 179384 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 179384 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 181781 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 181781 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 180863 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 180863 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 175534 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 175534 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 65697 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 65697 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 5280 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 5280 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 108708 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 108708 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 65705 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 65705 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 1137 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 1137 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 1137 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 1137 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 1137 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 1137 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 65715 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 65715 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 181277 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 181277 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 182449 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 182449 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 65714 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 65714 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 154352 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 154352 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 65688 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 65688 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 65706 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 65706 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 179187 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 179187 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 179902 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 179902 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 180359 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 180359 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 160922 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 160922 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 61567 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 61567 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 93748 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 93748 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 181086 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 181086 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 93690 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 93690 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 174322 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 174322 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 179615 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 179615 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 213213 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 106804 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 106804 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 106920 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 106920 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 65718 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 65718 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 179384 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 179384 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 180399 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 180399 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 182228 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 182228 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 6634 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 6634 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