Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Unit Assay Type Assay Description Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles
CHEMBL4094454 v1ar_human Human No 10.5 EC50 = 0.0 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
1034 19 14 15 -4.3 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](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL373742 v1ar_rat Rat Yes 10.2 EC50 = 0.1 nM Funct
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
None None None None
CHEMBL373742 v1ar_rat Rat Yes 10.2 EC50 = 0.1 nM Funct
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
None None None None
CHEMBL1819441 v1ar_rat Rat No 10.2 EC50 = 0.1 nM Funct
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
None None None N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1819441 v1ar_rat Rat No 10.1 EC50 = 0.1 nM Funct
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
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
CHEMBL1817706 v1ar_rat Rat No 10.0 EC50 = 0.1 nM Funct
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
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
CHEMBL1817706 v1ar_rat Rat No 10.0 EC50 = 0.1 nM Funct
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
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
CHEMBL4094454 v1ar_human Human No 9.9 EC50 = 0.1 nM Funct
Agonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
1034 19 14 15 -4.3 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](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819542 v1ar_rat Rat Yes 9.9 EC50 = 0.1 nM Funct
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
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819542 v1ar_rat Rat Yes 9.9 EC50 = 0.1 nM Funct
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
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
CHEMBL1817704 v1ar_rat Rat No 9.9 EC50 = 0.1 nM Funct
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
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
CHEMBL3342789 v1ar_human Human No 9.9 EC50 = 0.1 nM Funct
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
334 4 1 5 2.7 O=S(=O)(Nc1ccnn1-c1ccccn1)c1ccc(Cl)cc1
CHEMBL4165132 v1ar_human Human Yes 9.9 EC50 = 0.1 nM Funct
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
271 3 1 4 1.9 Cn1nccc1NS(=O)(=O)c1ccc(Cl)cc1
CHEMBL1817704 v1ar_rat Rat No 9.9 EC50 = 0.1 nM Funct
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
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
CHEMBL1819540 v1ar_human Human No 9.9 EC50 = 0.1 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1819540 v1ar_human Human No 9.9 EC50 = 0.1 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1819441 v1ar_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1819441 v1ar_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL3342790 v1ar_human Human No 9.8 EC50 = 0.2 nM Funct
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
368 4 1 5 3.1 O=S(=O)(Nc1ccnn1-c1ccccn1)c1ccc(C(F)(F)F)cc1
CHEMBL4173036 v1ar_human Human Yes 9.8 EC50 = 0.2 nM Funct
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
305 3 1 4 2.2 Cn1nccc1NS(=O)(=O)c1ccc(C(F)(F)F)cc1
CHEMBL1817707 v1ar_rat Rat No 9.8 EC50 = 0.2 nM Funct
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
None None None CCNCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1817707 v1ar_rat Rat No 9.8 EC50 = 0.2 nM Funct
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
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
CHEMBL4096848 v1ar_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
949 15 11 14 -3.6 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](C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL395429 v1ar_human Human Yes 9.7 EC50 = 0.2 nM Funct
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
None None None None
CHEMBL395429 v1ar_human Human Yes 9.7 EC50 = 0.2 nM Funct
Agonist activity at recombinant human V1a receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric methodAgonist activity at recombinant human V1a receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method
None None None None
CHEMBL1817706 v1ar_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CCCNCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1817706 v1ar_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CCCNCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1819541 v1ar_human Human No 9.6 EC50 = 0.2 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL373742 v1ar_human Human Yes 9.6 EC50 = 0.2 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None None
CHEMBL1819541 v1ar_human Human No 9.6 EC50 = 0.2 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL373742 v1ar_human Human Yes 9.6 EC50 = 0.2 nM Bind
Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
None None None None
CHEMBL373742 v1ar_human Human Yes 9.6 EC50 = 0.2 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None None
CHEMBL1819555 v1ar_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819555 v1ar_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817705 v1ar_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817705 v1ar_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819542 v1ar_human Human Yes 9.6 EC50 = 0.3 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819542 v1ar_human Human Yes 9.6 EC50 = 0.3 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817705 v1ar_rat Rat No 9.5 EC50 = 0.3 nM Funct
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
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
CHEMBL1817705 v1ar_rat Rat No 9.5 EC50 = 0.3 nM Funct
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
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
CHEMBL1817761 v1ar_rat Rat No 9.5 EC50 = 0.3 nM Funct
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
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
CHEMBL1817761 v1ar_rat Rat No 9.5 EC50 = 0.3 nM Funct
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
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
CHEMBL1817702 v1ar_rat Rat No 9.5 EC50 = 0.3 nM Funct
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
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
CHEMBL1817702 v1ar_rat Rat No 9.5 EC50 = 0.3 nM Funct
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
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
CHEMBL1819440 v1ar_rat Rat Yes 9.5 EC50 = 0.3 nM Funct
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
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
CHEMBL1819440 v1ar_rat Rat Yes 9.5 EC50 = 0.4 nM Funct
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
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
CHEMBL1817704 v1ar_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817704 v1ar_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL4070577 v1ar_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
1025 17 11 14 -2.3 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1819543 v1ar_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL4078856 v1ar_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
991 18 11 14 -2.4 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1819543 v1ar_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819548 v1ar_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819439 v1ar_rat Rat No 9.3 EC50 = 0.5 nM Funct
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
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
CHEMBL1819548 v1ar_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819439 v1ar_rat Rat No 9.3 EC50 = 0.5 nM Funct
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
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
CHEMBL1817709 v1ar_rat Rat Yes 9.3 EC50 = 0.5 nM Funct
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
None None None None
CHEMBL4065273 v1ar_human Human No 9.3 EC50 = 0.6 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
1019 20 11 14 -1.6 CCCCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL4101771 v1ar_human Human No 9.3 EC50 = 0.6 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
1019 20 11 14 -1.6 CCCCCCC(NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1817709 v1ar_rat Rat Yes 9.3 EC50 = 0.6 nM Funct
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
None None None None
CHEMBL1817707 v1ar_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CCNCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1817707 v1ar_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CCNCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1819549 v1ar_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccsc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819549 v1ar_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccsc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817756 v1ar_rat Rat No 9.2 EC50 = 0.6 nM Funct
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
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccco2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817756 v1ar_rat Rat No 9.2 EC50 = 0.6 nM Funct
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
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
CHEMBL4063150 v1ar_human Human No 9.2 EC50 = 0.7 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
965 16 12 15 -4.6 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](CO)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817761 v1ar_human Human No 9.2 EC50 = 0.7 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819440 v1ar_human Human Yes 9.2 EC50 = 0.7 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1817761 v1ar_human Human No 9.2 EC50 = 0.7 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819440 v1ar_human Human Yes 9.2 EC50 = 0.7 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1819554 v1ar_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819554 v1ar_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817708 v1ar_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNCCC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817708 v1ar_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNCCC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817702 v1ar_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCC(N)=O)NC1=O
CHEMBL1817702 v1ar_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCC(N)=O)NC1=O
CHEMBL1819556 v1ar_human Human No 9.0 EC50 = 0.9 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)C2(CCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819556 v1ar_human Human No 9.0 EC50 = 0.9 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)C2(CCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817754 v1ar_human Human No 9.0 EC50 = 1.0 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CCNCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1817754 v1ar_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CCNCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1817695 v1ar_rat Rat No 9.0 EC50 = 1 nM Funct
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
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
CHEMBL1819560 v1ar_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
1021 19 12 16 -4.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NOC)NC1=O
CHEMBL1819560 v1ar_human Human No 8.9 EC50 = 1.1 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
1021 19 12 16 -4.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NOC)NC1=O
CHEMBL4084223 v1ar_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
977 16 11 14 -2.9 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](C(=O)NCC(N)=O)C(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817752 v1ar_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4102192 v1ar_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
1031 17 11 14 -1.6 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](CC2CCCCC2)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817692 v1ar_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817752 v1ar_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817770 v1ar_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817770 v1ar_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817692 v1ar_human Human No 8.8 EC50 = 1.4 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL395429 v1ar_human Human Yes 8.8 EC50 = 1.5 nM Funct
Agonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
None None None None
CHEMBL1817755 v1ar_human Human No 8.8 EC50 = 1.5 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CCCNCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1817755 v1ar_human Human No 8.8 EC50 = 1.5 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CCCNCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1817772 v1ar_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817772 v1ar_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817695 v1ar_human Human No 8.8 EC50 = 1.7 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL1817695 v1ar_human Human No 8.8 EC50 = 1.7 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL1817749 v1ar_rat Rat No 8.7 EC50 = 2.0 nM Funct
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
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
CHEMBL395429 v1ar_human Human Yes 8.0 EC50 = 10 nM Bind
Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
None None None None
CHEMBL1817757 v1ar_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccco2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817769 v1ar_human Human No 8.0 EC50 = 10.5 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1819552 v1ar_human Human No 8.0 EC50 = 10.7 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC(C)(C)C)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL473106 v1ar_human Human Yes 5.0 EC50 = 10471 nM Funct
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))]
346 3 0 5 4.0 CCN1C(=S)SC(=O)C1=C1C=C(C)N(Cc2ccco2)C(C)=C1
CHEMBL439044 v1ar_human Human Yes 8.0 EC50 = 11 nM Funct
Agonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
991 17 11 14 -2.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817769 v1ar_human Human No 8.0 EC50 = 11 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1819552 v1ar_human Human No 8.0 EC50 = 11 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC(C)(C)C)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817762 v1ar_human Human No 7.9 EC50 = 11.5 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817691 v1ar_human Human No 7.9 EC50 = 11.8 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
1007 18 13 16 -4.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NO)NC1=O
CHEMBL1356933 v1ar_human Human Yes 5.0 EC50 = 11015 nM Funct
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))]
265 4 2 2 3.5 Oc1ccc(Cl)cc1CNCc1ccc(F)cc1
CHEMBL1616435 v1ar_human Human Yes 5.0 EC50 = 11015 nM Funct
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))]
265 4 2 2 3.5 Oc1ccc(Cl)cc1CNCc1ccc(F)cc1
CHEMBL3353940 v1ar_human Human No 7.9 EC50 = 12 nM Bind
Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1035 23 11 14 -1.1 CCCCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL1817691 v1ar_human Human No 7.9 EC50 = 12 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
1007 18 13 16 -4.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NO)NC1=O
CHEMBL1817762 v1ar_human Human No 7.9 EC50 = 12 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817767 v1ar_human Human No 7.9 EC50 = 12 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)C2(CCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817767 v1ar_human Human No 7.9 EC50 = 12.3 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)C2(CCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1819553 v1ar_human Human No 7.9 EC50 = 12.6 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL276711 v1ar_human Human Yes 4.9 EC50 = 12070 nM Funct
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))]
238 1 2 1 3.1 Cc1cc(C)c(/C=C2\C(=O)Nc3ccccc32)[nH]1
CHEMBL1390471 v1ar_human Human Yes 4.9 EC50 = 12729 nM Funct
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))]
404 9 2 5 4.0 COc1ccc(CCNCC(O)Cn2c3ccccc3c3ccccc32)cc1OC
CHEMBL1819553 v1ar_human Human No 7.9 EC50 = 13 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817763 v1ar_human Human No 7.9 EC50 = 13.8 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL603708 v1ar_human Human No 7.9 EC50 = 14 nM Bind
Activity at human vasopressin V1a receptor expressed in CHO cells by NFAT-luciferase gene reporter assayActivity at human vasopressin V1a receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL1817759 v1ar_human Human No 7.9 EC50 = 14 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccco2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817763 v1ar_human Human No 7.9 EC50 = 14 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817759 v1ar_human Human No 7.8 EC50 = 14.5 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccco2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817760 v1ar_human Human No 7.8 EC50 = 14.5 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817758 v1ar_human Human No 7.8 EC50 = 15 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccco2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817760 v1ar_human Human No 7.8 EC50 = 15 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817758 v1ar_human Human No 7.8 EC50 = 15.5 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccco2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1587205 v1ar_human Human Yes 4.8 EC50 = 15075 nM Funct
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))]
425 5 1 5 4.7 N=c1n(CC(=O)c2ccc(Br)s2)c2ccccc2n1Cc1ccccc1
CHEMBL1625302 v1ar_human Human Yes 4.8 EC50 = 15075 nM Funct
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))]
425 5 1 5 4.7 N=c1n(CC(=O)c2ccc(Br)s2)c2ccccc2n1Cc1ccccc1
CHEMBL1817699 v1ar_human Human No 7.8 EC50 = 16 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL1817699 v1ar_human Human No 7.8 EC50 = 16.2 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL1437791 v1ar_human Human No 4.8 EC50 = 17545 nM Funct
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))]
282 4 2 3 3.4 Oc1ccc(Cl)cc1CNCc1ccc(Cl)nc1
CHEMBL3211384 v1ar_human Human No 4.8 EC50 = 17545 nM Funct
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))]
282 4 2 3 3.4 Oc1ccc(Cl)cc1CNCc1ccc(Cl)nc1
CHEMBL1817671 v1ar_human Human No 7.8 EC50 = 18 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCC(N)=O)NC1=O
CHEMBL1817671 v1ar_human Human No 7.7 EC50 = 18.2 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCC(N)=O)NC1=O
CHEMBL1819547 v1ar_human Human No 7.7 EC50 = 18.6 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cscn2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3189462 v1ar_human Human Yes 4.7 EC50 = 18605 nM Funct
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))]
379 6 2 6 2.0 CCN(CC)c1ccc2cc(C(N)=O)/c(=N\NC(=O)c3ccncc3)oc2c1
CHEMBL3353938 v1ar_human Human No 7.7 EC50 = 19 nM Bind
Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1021 22 11 14 -1.5 CCCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL1819547 v1ar_human Human No 7.7 EC50 = 19 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cscn2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817749 v1ar_rat Rat No 8.7 EC50 = 2 nM Funct
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
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
CHEMBL1817698 v1ar_human Human No 8.7 EC50 = 2.1 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL1819555 v1ar_rat Rat No 8.7 EC50 = 2.1 nM Funct
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
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
CHEMBL1817698 v1ar_human Human No 8.7 EC50 = 2.1 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL1819555 v1ar_rat Rat No 8.7 EC50 = 2.1 nM Funct
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
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
CHEMBL4474284 v1ar_human Human No 8.7 EC50 = 2.2 nM Funct
Agonist activity at recombinant human V1a receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric methodAgonist activity at recombinant human V1a receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method
1074 20 12 15 -2.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819550 v1ar_human Human No 8.7 EC50 = 2.2 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccco2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819550 v1ar_human Human No 8.7 EC50 = 2.2 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccco2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3301668 v1ar_human Human Yes 8.6 EC50 = 2.3 nM Funct
Agonist activity at recombinant human V1a receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric methodAgonist activity at recombinant human V1a receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method
None None None CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C
CHEMBL1817709 v1ar_human Human Yes 8.6 EC50 = 2.4 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None None
CHEMBL1817753 v1ar_human Human No 8.6 EC50 = 2.4 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4084795 v1ar_human Human No 8.6 EC50 = 2.4 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
1025 17 11 14 -2.3 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](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817709 v1ar_human Human Yes 8.6 EC50 = 2.4 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None None
CHEMBL1817753 v1ar_human Human No 8.6 EC50 = 2.4 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817756 v1ar_human Human No 8.6 EC50 = 2.6 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccco2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817756 v1ar_human Human No 8.6 EC50 = 2.6 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccco2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817751 v1ar_human Human No 8.6 EC50 = 2.7 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
991 17 12 15 -4.8 CCNC(=O)C[C@@H]1NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817751 v1ar_human Human No 8.6 EC50 = 2.7 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
991 17 12 15 -4.8 CCNC(=O)C[C@@H]1NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817698 v1ar_rat Rat No 8.6 EC50 = 2.7 nM Funct
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
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
CHEMBL1817698 v1ar_rat Rat No 8.6 EC50 = 2.8 nM Funct
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
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
CHEMBL1817749 v1ar_human Human No 8.5 EC50 = 2.9 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817749 v1ar_human Human No 8.5 EC50 = 2.9 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1819559 v1ar_human Human No 7.7 EC50 = 20.9 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
1047 20 12 15 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NCC(C)C)NC1=O
CHEMBL1549574 v1ar_human Human Yes 4.7 EC50 = 20837 nM Funct
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))]
402 5 2 3 5.1 COc1ccc(C2NCCc3c2[nH]c2ccccc32)cc1COc1ccc(F)cc1
CHEMBL1624349 v1ar_human Human Yes 4.7 EC50 = 20837 nM Funct
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))]
402 5 2 3 5.1 COc1ccc(C2NCCc3c2[nH]c2ccccc32)cc1COc1ccc(F)cc1
CHEMBL439044 v1ar_human Human Yes 7.7 EC50 = 21 nM Bind
Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
991 17 11 14 -2.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819559 v1ar_human Human No 7.7 EC50 = 21 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
1047 20 12 15 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NCC(C)C)NC1=O
CHEMBL1339676 v1ar_human Human Yes 4.7 EC50 = 21340 nM Funct
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))]
330 1 1 3 4.0 Clc1ccc2c(c1)C(N1CCNCC1)Cc1ccccc1S2
CHEMBL1618211 v1ar_human Human Yes 4.7 EC50 = 21340 nM Funct
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))]
330 1 1 3 4.0 Clc1ccc2c(c1)C(N1CCNCC1)Cc1ccccc1S2
CHEMBL4094019 v1ar_human Human No 7.6 EC50 = 23 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
976 16 10 13 -0.8 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](CC(C)C)NC1=O
CHEMBL1559201 v1ar_human Human No 5.6 EC50 = 2325 nM Funct
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))]
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
CHEMBL395429 v1ar_human Human Yes 6.6 EC50 = 260 nM Funct
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
None None None None
CHEMBL1817703 v1ar_human Human No 7.5 EC50 = 29.5 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819545 v1ar_human Human No 7.5 EC50 = 29.5 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL4065273 v1ar_human Human No 8.5 EC50 = 3.1 nM Funct
Agonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
1019 20 11 14 -1.6 CCCCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL4101771 v1ar_human Human No 8.5 EC50 = 3.1 nM Funct
Agonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
1019 20 11 14 -1.6 CCCCCCC(NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL439044 v1ar_human Human Yes 8.5 EC50 = 3.2 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
991 17 11 14 -2.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817771 v1ar_human Human No 8.5 EC50 = 3.2 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817771 v1ar_human Human No 8.5 EC50 = 3.2 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817693 v1ar_human Human No 8.5 EC50 = 3.5 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL1817693 v1ar_human Human No 8.4 EC50 = 3.6 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL1817750 v1ar_human Human No 8.4 EC50 = 3.9 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
977 16 12 15 -5.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)NC)NC1=O
CHEMBL4083700 v1ar_human Human No 8.4 EC50 = 3.9 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
991 17 11 14 -2.5 CC(C)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
CHEMBL1817750 v1ar_human Human No 8.4 EC50 = 3.9 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
977 16 12 15 -5.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)NC)NC1=O
CHEMBL1817703 v1ar_human Human No 7.5 EC50 = 30 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819545 v1ar_human Human No 7.5 EC50 = 30 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL24781 v1ar_human Human Yes 5.5 EC50 = 3200 nM Bind
Activity at human vasopressin V1a receptor expressed in CHO cells by NFAT-luciferase gene reporter assayActivity at human vasopressin V1a receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C
CHEMBL1819558 v1ar_human Human No 7.4 EC50 = 38.9 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
1019 19 12 15 -4.0 CCNC(=O)CC[C@@H]1NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1819558 v1ar_human Human No 7.4 EC50 = 39 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
1019 19 12 15 -4.0 CCNC(=O)CC[C@@H]1NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4095930 v1ar_human Human No 8.4 EC50 = 4 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
1005 17 11 14 -2.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCCCC2C(=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
CHEMBL4458988 v1ar_human Human No 8.4 EC50 = 4 nM Funct
Agonist activity at recombinant human V1a receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric methodAgonist activity at recombinant human V1a receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method
1056 20 12 14 -2.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](N)CCSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817696 v1ar_human Human No 8.4 EC50 = 4.1 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
993 17 13 16 -5.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)NO)NC1=O
CHEMBL1817696 v1ar_human Human No 8.4 EC50 = 4.1 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
993 17 13 16 -5.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)NO)NC1=O
CHEMBL1819554 v1ar_rat Rat No 8.4 EC50 = 4.2 nM Funct
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
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
CHEMBL4096848 v1ar_human Human No 8.4 EC50 = 4.2 nM Funct
Agonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
949 15 11 14 -3.6 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](C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1819554 v1ar_rat Rat No 8.4 EC50 = 4.2 nM Funct
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
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
CHEMBL4078856 v1ar_human Human No 8.4 EC50 = 4.4 nM Funct
Agonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
991 18 11 14 -2.4 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
CHEMBL1817701 v1ar_human Human No 8.3 EC50 = 4.8 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL1817751 v1ar_rat Rat No 8.3 EC50 = 4.8 nM Funct
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
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
CHEMBL1817701 v1ar_human Human No 8.3 EC50 = 4.8 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL1817751 v1ar_rat Rat No 8.3 EC50 = 4.8 nM Funct
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
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
CHEMBL3301668 v1ar_human Human Yes 7.4 EC50 = 41 nM Bind
Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
None None None CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C
CHEMBL439044 v1ar_human Human Yes 7.4 EC50 = 41 nM Funct
Agonist activity at vasopressin 1a receptor (unknown origin)Agonist activity at vasopressin 1a receptor (unknown origin)
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
CHEMBL3276119 v1ar_human Human No 7.4 EC50 = 45 nM Funct
Agonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
973 17 11 13 -2.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[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
CHEMBL363910 v1ar_human Human Yes 6.3 EC50 = 465 nM Bind
Activity at human vasopressin V1a receptor expressed in CHO cells by NFAT-luciferase gene reporter assayActivity at human vasopressin V1a receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2
CHEMBL1479813 v1ar_human Human Yes 5.3 EC50 = 4675 nM Funct
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))]
384 6 2 5 3.2 CC(NC(=O)Nc1ccc([N+](=O)[O-])cc1)C(c1ccccc1)N1CCOCC1
CHEMBL1492232 v1ar_human Human Yes 5.3 EC50 = 4753 nM Funct
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))]
324 3 1 4 2.4 O=C1c2cccc3c(N4CCCCC4)ccc(c23)C(=O)N1CCO
CHEMBL4084223 v1ar_human Human No 8.3 EC50 = 5.1 nM Funct
Agonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
977 16 11 14 -2.9 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](C(=O)NCC(N)=O)C(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817700 v1ar_human Human No 8.3 EC50 = 5.1 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL1817700 v1ar_human Human No 8.3 EC50 = 5.2 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL1817694 v1ar_human Human No 8.2 EC50 = 5.7 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL1817694 v1ar_human Human No 8.2 EC50 = 5.8 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL395429 v1ar_human Human Yes 8.2 EC50 = 5.8 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
None None None None
CHEMBL1819544 v1ar_human Human No 6.3 EC50 = 510 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL1819544 v1ar_human Human No 6.3 EC50 = 512.9 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL1817770 v1ar_rat Rat No 7.2 EC50 = 57 nM Funct
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
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817770 v1ar_rat Rat No 7.2 EC50 = 57.5 nM Funct
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
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
CHEMBL1819557 v1ar_human Human No 8.2 EC50 = 6 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
1005 18 12 15 -4.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NC)NC1=O
CHEMBL1819557 v1ar_human Human No 8.2 EC50 = 6.0 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
1005 18 12 15 -4.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NC)NC1=O
CHEMBL3276119 v1ar_human Human No 8.2 EC50 = 6.5 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
973 17 11 13 -2.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[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
CHEMBL395429 v1ar_human Human Yes 7.2 EC50 = 60 nM Funct
Agonist activity at C-terminal GFP-tagged V1a receptor (unknown origin) expressed in HEK293 cells measured after 18 hrs by luciferase reporter gene assayAgonist activity at C-terminal GFP-tagged V1a receptor (unknown origin) expressed in HEK293 cells measured after 18 hrs by luciferase reporter gene assay
None None None None
CHEMBL1584768 v1ar_human Human Yes 5.2 EC50 = 6229 nM Funct
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))]
407 5 2 3 4.6 CC(NC(=O)Nc1ccc(Cl)c(Cl)c1)C(c1ccccc1)N1CCOCC1
CHEMBL4444891 v1ar_human Human No 6.2 EC50 = 650 nM Funct
Agonist activity at recombinant human V1a receptor expressed in HEK293 cells measured after 5 hrs by luciferase reporter gene assayAgonist activity at recombinant human V1a receptor expressed in HEK293 cells measured after 5 hrs by luciferase reporter gene assay
885 13 9 12 -0.4 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCCCCN)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1341433 v1ar_human Human Yes 5.2 EC50 = 6678 nM Funct
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))]
350 1 1 4 3.7 O=c1c2cc(Br)ccc2nc(-c2cccc(Cl)c2)n1O
CHEMBL4100627 v1ar_human Human No 7.2 EC50 = 69 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
934 14 10 13 -1.8 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](C)NC1=O
CHEMBL1817690 v1ar_human Human No 7.2 EC50 = 69 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
1035 19 11 16 -4.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)N(C)OC)NC1=O
CHEMBL1817690 v1ar_human Human No 7.2 EC50 = 69.2 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
1035 19 11 16 -4.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)N(C)OC)NC1=O
CHEMBL1817764 v1ar_human Human No 8.1 EC50 = 7.2 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccsc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL4104080 v1ar_human Human No 8.1 EC50 = 7.3 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
992 15 12 14 -2.4 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)NNC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817764 v1ar_human Human No 8.1 EC50 = 7.3 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccsc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817765 v1ar_human Human No 8.1 EC50 = 7.4 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccsc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817765 v1ar_human Human No 8.1 EC50 = 7.4 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccsc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817768 v1ar_human Human No 8.1 EC50 = 7.7 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL395429 v1ar_human Human Yes 8.1 EC50 = 7.7 nM Funct
Agonist activity at vasopressin 1a receptor (unknown origin)Agonist activity at vasopressin 1a receptor (unknown origin)
None None None None
CHEMBL1817768 v1ar_human Human No 8.1 EC50 = 7.8 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817766 v1ar_human Human No 8.1 EC50 = 7.9 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)C2(CCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817697 v1ar_human Human No 8.1 EC50 = 7.9 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL1817766 v1ar_human Human No 8.1 EC50 = 7.9 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
None None None CC[C@H](C)[C@@H]1NC(=O)C2(CCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O
CHEMBL1817754 v1ar_rat Rat No 8.1 EC50 = 7.9 nM Funct
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
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
CHEMBL4104080 v1ar_human Human No 7.2 EC50 = 70 nM Funct
Agonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1a receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
992 15 12 14 -2.4 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)NNC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354592 v1ar_human Human No 7.2 EC50 = 71 nM Bind
Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1038 20 11 13 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccc(C)c2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3353956 v1ar_human Human No 7.1 EC50 = 75 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
1047 20 11 15 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccs2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817697 v1ar_human Human No 8.1 EC50 = 8 nM Funct
Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
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
CHEMBL1817754 v1ar_rat Rat No 8.1 EC50 = 8 nM Funct
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
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
CHEMBL1817692 v1ar_rat Rat No 8.1 EC50 = 8.1 nM Funct
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
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
CHEMBL4070222 v1ar_human Human No 8.1 EC50 = 8.2 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
1007 17 12 15 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2C[C@@H](O)C[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1817692 v1ar_rat Rat No 8.1 EC50 = 8.2 nM Funct
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
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
CHEMBL4101586 v1ar_human Human No 8.1 EC50 = 8.9 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
950 15 11 14 -2.8 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](CO)NC1=O
CHEMBL2004487 v1ar_human Human No 5.1 EC50 = 8366 nM Funct
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))]
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
CHEMBL3353932 v1ar_human Human No 7.1 EC50 = 85 nM Bind
Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1005 19 11 14 -2.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C2CCC2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354585 v1ar_human Human No 7.1 EC50 = 86 nM Bind
Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1004 22 11 13 -1.8 CCCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL4063521 v1ar_human Human No 8.1 EC50 = 9 nM Funct
Agonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human V1b receptor expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
1019 18 13 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](CCCNC(=N)N)NC1=O
CHEMBL395429 v1ar_human Human Yes 8.1 EC50 = 9 nM Funct
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
None None None None
CHEMBL1837039 v1ar_human Human No 9.3 IC50 = 0.5 nM Funct
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
487 4 0 7 2.8 CN(C)S(=O)(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1
CHEMBL2370569 v1ar_human Human Yes 9.2 IC50 = 0.6 nM Bind
Binding affinity to human vasopressin V1a receptor by radioligand displacement assayBinding affinity to human vasopressin V1a receptor by radioligand displacement assay
None None None COc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1
CHEMBL2370569 v1ar_human Human Yes 9.0 IC50 = 1.0 nM Bind
Displacement of [3H]AVP from human recombinant V1a receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]AVP from human recombinant V1a receptor expressed in CHO cells measured after 60 mins by scintillation counting method
None None None COc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1
CHEMBL2370569 v1ar_human Human Yes 9.0 IC50 = 1.0 nM Bind
Displacement of [3H]AVP from human recombinant arginine vasopressin receptor 1a expressed in CHO cellsDisplacement of [3H]AVP from human recombinant arginine vasopressin receptor 1a expressed in CHO cells
None None None COc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1
CHEMBL3976964 v1ar_human Human No 9.0 IC50 = 1 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
609 10 3 8 3.3 NC(=O)OCC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1C(F)(F)F
CHEMBL4799793 v1ar_human Human No 9.0 IC50 = 1 nM Funct
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
394 3 0 5 4.9 Clc1ccc2c(c1)CCCc1nnc([C@H]3CC[C@H](Oc4ccccn4)CC3)n1-2
CHEMBL4128926 v1ar_human Human No 9.0 IC50 = 1.1 nM Bind
Displacement of [3H]AVP from human recombinant V1a receptor after 60 mins by scintillation counting analysisDisplacement of [3H]AVP from human recombinant V1a receptor after 60 mins by scintillation counting analysis
583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12
CHEMBL1837041 v1ar_human Human No 8.9 IC50 = 1.3 nM Funct
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
458 3 0 7 3.0 CS(=O)(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1
CHEMBL4799412 v1ar_human Human No 8.9 IC50 = 1.3 nM Funct
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
438 3 0 5 5.0 Brc1ccc2c(c1)CCCc1nnc([C@H]3CC[C@H](Oc4ccccn4)CC3)n1-2
CHEMBL4756031 v1ar_human Human No 8.8 IC50 = 1.7 nM Funct
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
426 2 0 5 5.3 Cc1cc([C@H]2CC[C@H](c3nnc4n3-c3ccc(Br)cc3CCC4)CC2)no1
CHEMBL2370569 v1ar_human Human Yes 8.7 IC50 = 1.9 nM Bind
Binding affinity to human vasopressin V1a receptor by radioligand displacement assayBinding affinity to human vasopressin V1a receptor by radioligand displacement assay
None None None COc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1
CHEMBL4789306 v1ar_human Human No 8.0 IC50 = 10 nM Funct
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
438 2 0 3 4.1 Cc1ccccc1N1CCN(C(=O)N2CN(C(=O)C3CC3)Cc3cc(Cl)ccc32)CC1
CHEMBL397187 v1ar_human Human No 8.0 IC50 = 10 nM Bind
Binding affinity for human cloned vasopressin V1a receptor expressed in CHO cellsBinding affinity for human cloned vasopressin V1a receptor expressed in CHO cells
568 9 1 6 5.0 CC(C)(C)C(O)C(C(=O)OCc1ccccc1)N1C(=O)[C@@H](N2C(=O)OC[C@@H]2c2ccccc2)[C@H]1/C=C/c1ccccc1
CHEMBL104839 v1ar_human Human No 8.0 IC50 = 10 nM Bind
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V1a receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V1a receptor
608 7 2 4 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCCC4)CC3)Cc3ccccc32)cc1
CHEMBL3900528 v1ar_human Human No 8.0 IC50 = 10 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
557 9 2 7 4.2 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(Cc2ccccc2F)c1=O)c1ccccc1Cl
CHEMBL302709 v1ar_rat Rat No 8.0 IC50 = 10 nM Bind
Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.
441 3 1 3 5.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1Cl
CHEMBL100402 v1ar_human Human No 8.0 IC50 = 10 nM Bind
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptor
451 3 2 3 5.8 Nc1ccc(C(=O)Nc2ccc(C(=O)N3CCC4(C=CCCC4)Cc4ccccc43)cc2)cc1
CHEMBL101157 v1ar_human Human No 8.0 IC50 = 10 nM Bind
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptor
454 3 1 2 6.4 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1F
CHEMBL440147 v1ar_human Human No 8.0 IC50 = 10 nM Bind
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptor
450 3 1 2 6.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1
CHEMBL302709 v1ar_rat Rat No 8.0 IC50 = 10 nM Bind
Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
441 3 1 3 5.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1Cl
CHEMBL293905 v1ar_rat Rat No 7.0 IC50 = 100 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
449 9 1 4 4.2 NCCCCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL4204210 v1ar_human Human Yes 7.0 IC50 = 100 nM Funct
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
531 4 2 6 4.2 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N(C)C
CHEMBL245086 v1ar_human Human No 7.0 IC50 = 100 nM Bind
Binding affinity for human cloned vasopressin V1a receptor expressed in CHO cellsBinding affinity for human cloned vasopressin V1a receptor expressed in CHO cells
586 10 0 6 5.5 O=C(OCc1ccccc1)C(C(=O)c1ccccc1)N1C(=O)[C@@H](N2C(=O)OC[C@@H]2c2ccccc2)[C@H]1/C=C/c1ccccc1
CHEMBL298911 v1ar_rat Rat No 7.0 IC50 = 100 nM Bind
Displacement of (Phe-3,4,5 [3H]-) AVP from isolated rat hepatic V1a receptorDisplacement of (Phe-3,4,5 [3H]-) AVP from isolated rat hepatic V1a receptor
476 3 1 4 5.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(Cl)ccc1Cl
CHEMBL248733 v1ar_human Human No 7.0 IC50 = 100 nM Bind
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cells
518 4 2 3 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(CO)CC3)Cc3ccccc32)c(Cl)c1
CHEMBL400048 v1ar_human Human No 7.0 IC50 = 100 nM Bind
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cells
484 4 2 3 5.5 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2
CHEMBL4745524 v1ar_human Human No 7.0 IC50 = 100 nM Funct
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
368 2 0 5 4.8 Cc1cc([C@H]2CC[C@H](c3nnc4n3-c3ccc(Cl)cc3CC4)CC2)no1
CHEMBL4787124 v1ar_human Human No 6.0 IC50 = 1000 nM Funct
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
371 1 1 4 3.3 C[C@H]1CN(C(=O)N2CCNc3cc(Cl)ccc32)CCN1c1ccccn1
CHEMBL389091 v1ar_human Human No 6.0 IC50 = 1000 nM Bind
Binding affinity for human cloned vasopressin V1a receptor expressed in CHO cellsBinding affinity for human cloned vasopressin V1a receptor expressed in CHO cells
571 10 1 4 5.9 CC(C)C[C@@H](C(=O)NCc1ccccc1Cl)N1C(=O)[C@@H](N2C(=O)OC[C@@H]2c2ccccc2)[C@H]1/C=C/c1ccccc1
CHEMBL334082 v1ar_rat Rat No 6.0 IC50 = 1000 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
443 5 1 4 5.0 COc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)C)c3ccccc32)cc1
CHEMBL237772 v1ar_human Human No 6.0 IC50 = 1000 nM Bind
Displacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cellsDisplacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cells
489 3 1 3 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CC3C=CC(=O)N3Cc3ccccc32)c(Cl)c1
CHEMBL237987 v1ar_human Human No 6.0 IC50 = 1000 nM Bind
Displacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cellsDisplacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cells
426 5 3 3 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)Nc2ccccc2C(=O)O)c(Cl)c1
CHEMBL238206 v1ar_human Human No 6.0 IC50 = 1000 nM Bind
Displacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cellsDisplacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cells
505 7 3 4 5.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)Nc2ccccc2Cn2cccc2C(=O)O)c(Cl)c1
CHEMBL392363 v1ar_human Human No 6.0 IC50 = 1000 nM Bind
Displacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cellsDisplacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cells
489 3 1 3 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2C=C3CCC(=O)N3Cc3ccccc32)c(Cl)c1
CHEMBL332090 v1ar_rat Rat No 5.0 IC50 = 10000 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
370 3 1 2 4.8 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)cc1
CHEMBL4543809 v1ar_human Human No 5.0 IC50 = 10970 nM Funct
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
425 5 0 6 4.1 COc1ccc(-n2c(C3CC3)nnc2N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)cn1
CHEMBL4759676 v1ar_human Human No 8.0 IC50 = 11 nM Funct
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
466 2 0 3 4.9 Cc1ccccc1N1CCN(C(=O)N2CN(C(=O)C3CCCC3)Cc3cc(Cl)ccc32)CC1
CHEMBL4779447 v1ar_human Human No 8.0 IC50 = 11 nM Funct
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
440 2 0 3 4.4 Cc1ccccc1N1CCN(C(=O)N2CN(C(=O)C(C)C)Cc3cc(Cl)ccc32)CC1
CHEMBL300963 v1ar_rat Rat No 8.0 IC50 = 11 nM Bind
Displacement of (Phe-3,4,5 [3H]-) AVP from isolated rat hepatic V1a receptorDisplacement of (Phe-3,4,5 [3H]-) AVP from isolated rat hepatic V1a receptor
442 3 1 4 5.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1Cl
CHEMBL1837035 v1ar_human Human No 7.0 IC50 = 110 nM Funct
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
380 2 1 6 3.3 Clc1ccc2c(c1)CNCc1nnc(C3CCN(c4ccccn4)CC3)n1-2
CHEMBL4212928 v1ar_human Human No 7.0 IC50 = 110 nM Funct
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
462 5 3 7 2.6 COC(=O)CNC(=O)NCc1ccc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)cc1C
CHEMBL350089 v1ar_human Human No 7.0 IC50 = 110 nM Bind
In vitro binding affinity to human V1a receptorIn vitro binding affinity to human V1a receptor
442 3 1 3 6.1 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCCCc3sccc32)c(Cl)c1
CHEMBL20319 v1ar_rat Rat No 7.0 IC50 = 110 nM Bind
Inhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptorInhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptor
587 8 0 6 3.9 CN(C)CCSC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O
CHEMBL2112655 v1ar_rat Rat No 6.0 IC50 = 1100 nM Bind
Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O
CHEMBL294293 v1ar_rat Rat No 5.0 IC50 = 11000 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
324 2 0 3 2.9 O=C(c1ccco1)N1CCC(N2C(=O)CCc3ccccc32)CC1
CHEMBL59397 v1ar_rat Rat No 5.0 IC50 = 11000 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
377 3 1 3 2.4 NC(=O)c1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL118933 v1ar_rat Rat No 5.0 IC50 = 11000 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
357 3 1 3 3.9 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1cccnc1
CHEMBL3763951 v1ar_human Human No 6.0 IC50 = 1113 nM Funct
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
609 7 2 8 4.7 COc1cc(CN2CCN(C(=O)NCc3ccc(C(=O)N4Cc5cnn(C)c5Nc5ccccc54)cc3C)CC2)cc(OC)c1
CHEMBL3763951 v1ar_human Human No 6.0 IC50 = 1113 nM Funct
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
609 7 2 8 4.7 COc1cc(CN2CCN(C(=O)NCc3ccc(C(=O)N4Cc5cnn(C)c5Nc5ccccc54)cc3C)CC2)cc(OC)c1
CHEMBL336825 v1ar_human Human No 5.9 IC50 = 1140 nM Bind
Ability to displace [3H]arginine vasopressin in cloned human V1a receptorAbility to displace [3H]arginine vasopressin in cloned human V1a receptor
522 6 2 4 6.6 O=C(O)C[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1
CHEMBL131439 v1ar_human Human No 5.9 IC50 = 1150 nM Bind
Ability to displace [3H]arginine vasopressin in cloned human V1a receptorAbility to displace [3H]arginine vasopressin in cloned human V1a receptor
572 7 2 5 6.4 O=C(Nc1ccc(C(=O)N2CCC(CCS(=O)(=O)O)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL249133 v1ar_human Human No 4.9 IC50 = 11600 nM Funct
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
528 5 2 4 5.8 COc1cc(NC(=O)c2cc(F)ccc2C)ccc1C(=O)N1CCC2(C=C(C(=O)O)CC2)Cc2ccccc21
CHEMBL1837018 v1ar_human Human No 6.9 IC50 = 117 nM Funct
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
333 4 0 5 3.4 Cc1nnc(C2CCN(c3ccccn3)CC2)n1Cc1ccccc1
CHEMBL4764976 v1ar_human Human No 6.9 IC50 = 117 nM Funct
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
345 2 0 5 3.5 c1ccc(N2CCC(c3nnc4n3-c3ccccc3CCC4)CC2)nc1
CHEMBL3953766 v1ar_human Human No 7.9 IC50 = 12 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
555 8 2 9 2.7 NC(=O)Cn1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nc1-c1ccccc1Cl
CHEMBL3924331 v1ar_human Human No 7.9 IC50 = 12 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
575 10 3 8 2.9 NC(=O)OCC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1Cl
CHEMBL100893 v1ar_human Human No 7.9 IC50 = 12 nM Bind
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptor
470 3 1 2 6.9 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1Cl
CHEMBL196737 v1ar_human Human No 7.9 IC50 = 12 nM Bind
Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor
406 4 0 2 6.3 CCCc1ccc(-c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)cc1
CHEMBL303134 v1ar_rat Rat No 6.9 IC50 = 120 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
491 10 1 4 4.3 CC(=O)NCCCCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL3942564 v1ar_human Human No 6.9 IC50 = 120 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
543 6 1 7 5.1 O=c1n(Cc2cc(-c3cccc(Cl)c3Cl)ncn2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F
CHEMBL3986461 v1ar_human Human No 6.9 IC50 = 120 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
499 6 1 8 4.0 O=c1n(Cc2nnc(-c3ccccc3Cl)o2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F
CHEMBL81133 v1ar_human Human No 6.9 IC50 = 120 nM Bind
Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.
453 3 1 3 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(C)c1
CHEMBL68948 v1ar_rat Rat No 6.9 IC50 = 120 nM Bind
Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1cc(Cl)ccc1Cl
CHEMBL64811 v1ar_rat Rat No 5.9 IC50 = 1200 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
368 2 0 2 3.9 O=C(c1ccc(Cl)cc1)N1CCC(N2C(=O)CCc3ccccc32)CC1
CHEMBL128687 v1ar_human Human No 5.9 IC50 = 1200 nM Bind
Ability to displace [3H]arginine vasopressin in cloned human V1a receptorAbility to displace [3H]arginine vasopressin in cloned human V1a receptor
521 6 1 4 6.7 CN(C)CC1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1
CHEMBL3353956 v1ar_human Human No 5.9 IC50 = 1200 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1047 20 11 15 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccs2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354594 v1ar_human Human No 5.9 IC50 = 1200 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1041 20 11 13 -1.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354602 v1ar_human Human No 5.9 IC50 = 1200 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1013 20 10 13 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccs2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL118863 v1ar_rat Rat No 5.9 IC50 = 1200 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
455 6 1 3 6.1 CCCN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21
CHEMBL332060 v1ar_rat Rat No 5.9 IC50 = 1200 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
386 3 1 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCOc3ccccc32)cc1
CHEMBL60773 v1ar_rat Rat No 4.9 IC50 = 12000 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
348 3 0 2 3.2 O=C(Cc1ccccc1)N1CCC(N2C(=O)CCc3ccccc32)CC1
CHEMBL2112651 v1ar_rat Rat No 4.9 IC50 = 12000 nM Bind
Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O
CHEMBL49429 v1ar_human Human Yes 6.9 IC50 = 124 nM Bind
Displacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cellsDisplacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cells
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL162748 v1ar_rat Rat No 4.9 IC50 = 12400 nM Bind
In vitro binding affinity for rat V1a receptorIn vitro binding affinity for rat V1a receptor
480 3 2 4 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)c(Cl)c1
CHEMBL163 v1ar_human Human Yes 4.9 IC50 = 12416 nM Bind
DRUGMATRIX: Vasopressin V1A radioligand binding (ligand: [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr)DRUGMATRIX: Vasopressin V1A radioligand binding (ligand: [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr)
720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1
CHEMBL106293 v1ar_human Human No 6.9 IC50 = 126 nM Funct
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
554 7 2 4 5.1 CN(C)CCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2
CHEMBL413711 v1ar_human Human No 6.9 IC50 = 128 nM Bind
Binding affinity for human cloned vasopressin V1a receptor expressed in CHO cellsBinding affinity for human cloned vasopressin V1a receptor expressed in CHO cells
537 10 1 4 5.2 CC(C)C[C@@H](C(=O)NCc1ccccc1)N1C(=O)[C@@H](N2C(=O)OC[C@@H]2c2ccccc2)[C@H]1/C=C/c1ccccc1
CHEMBL419667 v1ar_human Human Yes 7.9 IC50 = 13 nM Funct
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
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
CHEMBL3915616 v1ar_human Human No 7.9 IC50 = 13 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
651 9 3 8 5.0 CC(C)(C)OC(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(Cl)c1Cl
CHEMBL249340 v1ar_human Human No 7.9 IC50 = 13 nM Bind
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cells
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
CHEMBL4746716 v1ar_human Human No 7.9 IC50 = 13 nM Funct
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
423 2 0 5 4.3 Brc1ccc2c(c1)CCCc1nnc(C3CCN(c4ccccn4)CC3)n1-2
CHEMBL197616 v1ar_human Human No 7.9 IC50 = 13 nM Bind
Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor
370 2 0 3 5.4 O=C(c1ccc(-c2cccs2)cc1)N1Cc2cccn2Cc2ccccc21
CHEMBL371721 v1ar_human Human No 7.9 IC50 = 13 nM Bind
Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor
421 4 0 3 5.4 CN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(-c3ccccc3)cc1)C2
CHEMBL251771 v1ar_human Human No 6.9 IC50 = 130 nM Funct
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
498 4 1 4 5.6 COC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2
CHEMBL3954357 v1ar_human Human No 6.9 IC50 = 130 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
581 11 2 9 2.5 COCCn1c(-c2ccc(Cl)s2)nn(CC(=O)NCC(NS(C)(=O)=O)c2ccccc2C(F)(F)F)c1=O
CHEMBL60054 v1ar_rat Rat No 5.9 IC50 = 1300 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
350 2 1 3 3.0 O=C(c1ccc(O)cc1)N1CCC(N2C(=O)CCc3ccccc32)CC1
CHEMBL60262 v1ar_rat Rat No 5.9 IC50 = 1300 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
348 2 0 2 3.6 Cc1cccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)c1
CHEMBL3353933 v1ar_human Human No 5.9 IC50 = 1300 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1017 19 10 14 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCCSC[C@@H](C(=O)N2C[C@H](OC)C[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3353951 v1ar_human Human No 5.9 IC50 = 1300 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1042 20 11 15 -2.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccnc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354573 v1ar_human Human No 5.9 IC50 = 1300 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1048 21 12 15 -2.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCC2CCCN2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354596 v1ar_human Human No 5.9 IC50 = 1300 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1025 20 10 12 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL127686 v1ar_rat Rat No 5.9 IC50 = 1300 nM Bind
Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.
None None None None
CHEMBL338018 v1ar_rat Rat No 5.9 IC50 = 1300 nM Bind
Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H]2CCCCN2C1=O
CHEMBL405289 v1ar_rat Rat No 5.9 IC50 = 1300 nM Bind
Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.
None None None CCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O
CHEMBL119638 v1ar_rat Rat No 5.9 IC50 = 1300 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
481 4 1 3 6.3 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccc(Cl)cc3Cl)cc2)c2ccccc21
CHEMBL2112894 v1ar_rat Rat No 5.9 IC50 = 1300 nM Bind
Displacement of [3H]AVP from binding to arginine vasopressin 1a (V1a) column of rat liverDisplacement of [3H]AVP from binding to arginine vasopressin 1a (V1a) column of rat liver
610 12 1 7 2.9 CCN(CC)[C@@H](CCS(C)(=O)=O)C(=O)N[C@H]1CC2CC[C@]1(CS(=O)(=O)N1CCN(c3ccccc3C)CC1)C2(C)C
CHEMBL20002 v1ar_rat Rat No 5.9 IC50 = 1300 nM Bind
Inhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptorInhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptor
542 5 0 6 3.2 CC(=O)OC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O
CHEMBL20171 v1ar_rat Rat No 5.9 IC50 = 1300 nM Bind
Inhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptorInhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptor
557 7 1 6 2.5 CN(CCO)C1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O
CHEMBL1837012 v1ar_human Human No 6.9 IC50 = 133 nM Funct
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
349 4 0 6 3.4 COc1ccc(-n2c(C)nnc2C2CCN(c3ccccn3)CC2)cc1
CHEMBL1837030 v1ar_human Human No 6.9 IC50 = 135 nM Funct
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
377 3 0 7 3.1 COc1ccc2c(c1)COCc1nnc(C3CCN(c4ccccn4)CC3)n1-2
CHEMBL4763639 v1ar_human Human No 6.9 IC50 = 135 nM Funct
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
439 3 0 3 4.1 Cc1ccccc1N1CCN(C(=O)C2CN(C(=O)C(C)C)Cc3cc(Cl)ccc32)CC1
CHEMBL319636 v1ar_human Human No 6.9 IC50 = 135 nM Funct
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
569 6 2 5 5.0 COC(=O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3C)cc1)c1ccccc1C2
CHEMBL4126100 v1ar_human Human No 7.9 IC50 = 14 nM Funct
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
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
CHEMBL3937650 v1ar_human Human No 7.9 IC50 = 14 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
545 9 2 7 3.9 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(CCC(F)(F)F)c1=O)c1ccccc1Cl
CHEMBL128688 v1ar_human Human No 6.9 IC50 = 140 nM Bind
Ability to displace [3H]arginine vasopressin in cloned human V1a receptorAbility to displace [3H]arginine vasopressin in cloned human V1a receptor
536 7 2 4 7.0 O=C(O)CC[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1
CHEMBL118271 v1ar_rat Rat No 6.9 IC50 = 140 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
400 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3ccccc32)cc1
CHEMBL317919 v1ar_human Human No 6.9 IC50 = 140 nM Bind
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptor
464 3 1 2 6.9 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCC4(C=CCCC4)Cc4ccccc43)cc2)cc1C
CHEMBL60502 v1ar_rat Rat No 5.9 IC50 = 1400 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
352 2 0 2 3.4 O=C(c1ccc(F)cc1)N1CCC(N2C(=O)CCc3ccccc32)CC1
CHEMBL64332 v1ar_rat Rat No 5.9 IC50 = 1400 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
392 3 0 4 3.2 CC(=O)Oc1ccccc1C(=O)N1CCC(N2C(=O)CCc3ccccc32)CC1
CHEMBL4742335 v1ar_human Human No 5.9 IC50 = 1400 nM Funct
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
412 1 0 3 3.8 CC(=O)N1CCN(C(=O)N2CCN(c3ccccc3C)CC2)c2ccc(Cl)cc21
CHEMBL4757593 v1ar_human Human No 5.9 IC50 = 1400 nM Funct
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
370 1 1 3 3.8 Cc1ccccc1N1CCN(C(=O)N2CCNc3ccc(Cl)cc32)CC1
CHEMBL3353937 v1ar_human Human No 5.9 IC50 = 1400 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
947 19 11 13 -3.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCCSC[C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3353947 v1ar_human Human No 5.9 IC50 = 1400 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1055 20 11 14 -1.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(C)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354579 v1ar_human Human No 5.9 IC50 = 1400 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
991 21 12 14 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CCCO)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354588 v1ar_human Human No 5.9 IC50 = 1400 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1023 20 11 13 -1.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL420762 v1ar_rat Rat Yes 5.9 IC50 = 1400 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C
CHEMBL331164 v1ar_rat Rat No 5.9 IC50 = 1400 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
370 3 1 2 4.8 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1
CHEMBL4778700 v1ar_human Human No 5.9 IC50 = 1400 nM Funct
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
365 2 0 5 3.8 Clc1ccc2c(c1)CCc1nnc(C3CCN(c4ccccn4)CC3)n1-2
CHEMBL1790938 v1ar_rat Rat No 4.9 IC50 = 14000 nM Bind
Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.
None None None CC[C@@H](C)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)N(C)C(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O
CHEMBL333340 v1ar_rat Rat No 4.9 IC50 = 14000 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
400 5 1 3 4.9 CCOc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)cc1
CHEMBL1837021 v1ar_human Human No 5.8 IC50 = 1450 nM Funct
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
347 4 0 5 3.7 Cc1ccc(Cn2c(C)nnc2C2CCN(c3ccccn3)CC2)cc1
CHEMBL312036 v1ar_human Human No 7.8 IC50 = 15 nM Bind
Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.
469 4 1 4 5.4 COc1cc(NC(=O)c2cc(F)ccc2C)ccc1C(=O)N1Cc2cccn2Cc2ccccc21
CHEMBL418890 v1ar_human Human No 7.8 IC50 = 15 nM Bind
Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.
475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl
CHEMBL251771 v1ar_human Human No 7.8 IC50 = 15 nM Bind
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cells
498 4 1 4 5.6 COC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2
CHEMBL418890 v1ar_human Human No 7.8 IC50 = 15 nM Bind
In vitro binding affinity to human V1a receptorIn vitro binding affinity to human V1a receptor
475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl
CHEMBL101187 v1ar_human Human No 7.8 IC50 = 15 nM Bind
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptor
482 4 1 3 7.0 CSc1ccc(C(=O)Nc2ccc(C(=O)N3CCC4(C=CCCC4)Cc4ccccc43)cc2)cc1
CHEMBL49429 v1ar_human Human Yes 6.8 IC50 = 150 nM Bind
Binding affinity towards human V1a receptorsBinding affinity towards human V1a receptors
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL49429 v1ar_human Human Yes 6.8 IC50 = 150 nM Bind
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cells
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL307271 v1ar_rat Rat No 6.8 IC50 = 150 nM Bind
Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
432 3 1 2 6.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Cc3ccccc32)cc1
CHEMBL49429 v1ar_human Human Yes 6.8 IC50 = 150 nM Bind
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V1a receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V1a receptor
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL337725 v1ar_human Human No 6.8 IC50 = 150 nM Funct
Inhibition of vasopressin induced calcium immobilization in human V1a receptor expressing cellsInhibition of vasopressin induced calcium immobilization in human V1a receptor expressing cells
508 6 2 4 6.5 O=C(Nc1ccc(C(=O)N2CCC(CCO)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL305588 v1ar_rat Rat No 5.8 IC50 = 1500 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
350 2 1 3 3.0 O=C(c1ccccc1O)N1CCC(N2C(=O)CCc3ccccc32)CC1
CHEMBL431723 v1ar_rat Rat No 5.8 IC50 = 1500 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
434 8 0 3 5.2 CCCCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL3354572 v1ar_human Human No 5.8 IC50 = 1500 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1035 20 11 15 -2.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)CC2CCCO2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL71283 v1ar_rat Rat No 5.8 IC50 = 1500 nM Bind
Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
434 3 1 3 6.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Oc3ccccc32)cc1
CHEMBL283524 v1ar_rat Rat No 5.8 IC50 = 1500 nM Bind
Inhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptorInhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptor
500 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](O)C1=O)C2
CHEMBL107058 v1ar_human Human No 6.8 IC50 = 155 nM Funct
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
580 7 2 4 5.6 O=C(NCCN1CCCC1)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2
CHEMBL104839 v1ar_human Human No 7.8 IC50 = 16 nM Bind
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V1a receptor (Compound 7o)Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V1a receptor (Compound 7o)
608 7 2 4 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCCC4)CC3)Cc3ccccc32)cc1
CHEMBL159359 v1ar_rat Rat No 7.8 IC50 = 16 nM Bind
In vitro binding affinity for rat V1a receptorIn vitro binding affinity for rat V1a receptor
517 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1
CHEMBL316958 v1ar_human Human No 7.8 IC50 = 16 nM Bind
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptor
504 3 1 2 7.6 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl
CHEMBL301850 v1ar_rat Rat No 6.8 IC50 = 160 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
477 9 1 4 4.0 CC(=O)NCCCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL334363 v1ar_human Human No 6.8 IC50 = 160 nM Bind
Ability to displace [3H]arginine vasopressin in cloned human V1a receptorAbility to displace [3H]arginine vasopressin in cloned human V1a receptor
528 6 1 3 7.8 O=C(Nc1ccc(C(=O)N2CCC(CC(F)F)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL417458 v1ar_rat Rat No 6.8 IC50 = 160 nM Bind
Inhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptorInhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptor
570 8 1 6 2.8 CN(C)CCNC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O
CHEMBL3354590 v1ar_human Human No 5.8 IC50 = 1600 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1007 20 10 12 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL126765 v1ar_rat Rat No 5.8 IC50 = 1600 nM Bind
Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@H](CCCN)NC(=O)[C@H]2CCC=NN2C1=O
CHEMBL419793 v1ar_rat Rat No 5.8 IC50 = 1600 nM Bind
Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H]2CCCCN2C1=O
CHEMBL118660 v1ar_rat Rat Yes 5.8 IC50 = 1600 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
390 3 1 2 5.2 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccccc1Cl
CHEMBL118922 v1ar_rat Rat No 5.8 IC50 = 1600 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
427 5 2 3 5.3 CCNC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21
CHEMBL333139 v1ar_rat Rat Yes 5.8 IC50 = 1600 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
356 3 1 2 4.5 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccccc1
CHEMBL325819 v1ar_rat Rat No 4.8 IC50 = 16000 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
470 5 2 4 4.9 CC(=O)Nc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)C)c3ccccc32)cc1
CHEMBL331424 v1ar_rat Rat No 4.8 IC50 = 16000 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
401 4 1 4 4.4 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1cccc([N+](=O)[O-])c1
CHEMBL363910 v1ar_human Human Yes 5.8 IC50 = 1660 nM Funct
Antagonist activity at V1A receptor (unknown origin) by cAMP accumulation assayAntagonist activity at V1A receptor (unknown origin) by cAMP accumulation assay
402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2
CHEMBL1837022 v1ar_human Human No 7.8 IC50 = 17 nM Funct
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
375 7 0 5 4.4 CCCCc1nnc(C2CCN(c3ccccn3)CC2)n1Cc1ccccc1
CHEMBL1837031 v1ar_human Human No 7.8 IC50 = 17 nM Funct
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
381 2 0 6 3.7 Clc1ccc2c(c1)COCc1nnc(C3CCN(c4ccccn4)CC3)n1-2
CHEMBL3353935 v1ar_human Human No 7.8 IC50 = 17 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1017 19 11 14 -3.1 CCOc1ccc(C[C@@H]2NC(=O)CCCSC[C@@H](C(=O)N3C[C@@H](O)C[C@H]3C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]([C@@H](C)CC)NC2=O)cc1
CHEMBL3915055 v1ar_human Human No 7.8 IC50 = 17 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
548 6 1 7 5.5 O=c1n(Cc2cnc(-c3ccccc3C(F)(F)F)s2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F
CHEMBL3964694 v1ar_human Human No 7.8 IC50 = 17 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
560 9 4 7 2.5 NC(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1Cl
CHEMBL4743785 v1ar_human Human No 6.8 IC50 = 170 nM Funct
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
391 1 1 4 3.6 O=C(N1CCN(c2ncccc2Cl)CC1)N1CCNc2cc(Cl)ccc21
CHEMBL68033 v1ar_rat Rat No 6.8 IC50 = 170 nM Bind
Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
407 3 1 3 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3-c3ccccc32)cc1
CHEMBL278377 v1ar_rat Rat No 6.8 IC50 = 170 nM Bind
Inhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptorInhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptor
584 9 1 6 3.2 CN(C)CCCNC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O
CHEMBL3889504 v1ar_human Human No 5.8 IC50 = 1700 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
551 7 2 6 5.4 O=C(O)c1ccc(-c2ccccc2Cl)cc1Cn1nc(-c2ccc(Cl)cc2)n(CC(O)C(F)(F)F)c1=O
CHEMBL334009 v1ar_rat Rat No 5.8 IC50 = 1700 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
362 3 1 3 4.6 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccsc1
CHEMBL350090 v1ar_rat Rat No 5.8 IC50 = 1700 nM Bind
In vitro binding affinity for rat V1a receptorIn vitro binding affinity for rat V1a receptor
446 3 2 4 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1
CHEMBL351587 v1ar_human Human No 5.8 IC50 = 1740 nM Bind
In vitro binding affinity to human V1a receptorIn vitro binding affinity to human V1a receptor
442 3 1 5 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3cn(C)nc3-c3sccc32)cc1
CHEMBL114 v1ar_human Human Yes 4.8 IC50 = 17522 nM Bind
DRUGMATRIX: Vasopressin V1A radioligand binding (ligand: [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr)DRUGMATRIX: Vasopressin V1A radioligand binding (ligand: [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr)
670 12 5 7 3.1 CC(C)(C)NC(=O)[C@@H]1C[C@@H]2CCCC[C@@H]2CN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)c1ccc2ccccc2n1
CHEMBL4464246 v1ar_human Human No 5.8 IC50 = 1757 nM Funct
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
443 7 0 7 3.8 CCOCc1nnc(N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1
CHEMBL336825 v1ar_human Human No 5.8 IC50 = 1760 nM Funct
Inhibition of vasopressin induced calcium immobilization in human V1a receptor expressing cellsInhibition of vasopressin induced calcium immobilization in human V1a receptor expressing cells
522 6 2 4 6.6 O=C(O)C[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1
CHEMBL203513 v1ar_human Human No 5.8 IC50 = 1783 nM Bind
Displacement of [3H]AVP from human V1a receptor expressed in CHO cellsDisplacement of [3H]AVP from human V1a receptor expressed in CHO cells
415 2 1 5 5.0 Cn1ccc(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(Cl)c2)n1
CHEMBL1837027 v1ar_human Human No 7.8 IC50 = 18 nM Funct
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
400 6 0 8 2.7 c1ccc(Cn2c(Cn3nccn3)nnc2C2CCN(c3ccccn3)CC2)cc1
CHEMBL3907257 v1ar_human Human No 7.8 IC50 = 18 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
653 9 2 8 6.0 CC(C)(C)OC(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)s2)n(Cc2ccccc2F)c1=O)c1ccccc1C(F)(F)F
CHEMBL400267 v1ar_human Human No 7.8 IC50 = 18 nM Bind
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cells
541 6 2 3 7.1 CNCC1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL131566 v1ar_human Human No 6.8 IC50 = 180 nM Bind
Ability to displace [3H]arginine vasopressin in cloned human V1a receptorAbility to displace [3H]arginine vasopressin in cloned human V1a receptor
510 6 1 3 7.5 O=C(Nc1ccc(C(=O)N2CCC(CCF)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL4741743 v1ar_human Human No 6.8 IC50 = 180 nM Funct
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
437 3 0 3 3.8 Cc1ccccc1N1CCN(C(=O)C2CN(C(=O)C3CC3)Cc3cc(Cl)ccc32)CC1
CHEMBL49429 v1ar_human Human Yes 6.8 IC50 = 180 nM Bind
Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL3353942 v1ar_human Human No 5.8 IC50 = 1800 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1009 21 11 15 -3.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCOC)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL3354580 v1ar_human Human No 5.8 IC50 = 1800 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
991 21 12 14 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CCCO)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL333652 v1ar_rat Rat No 5.8 IC50 = 1800 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
399 3 1 3 4.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCN(C)Cc3ccccc32)cc1
CHEMBL277022 v1ar_rat Rat No 5.7 IC50 = 1850 nM Bind
Inhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptorInhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptor
571 7 1 7 2.4 COC(=O)CNC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O
CHEMBL4541860 v1ar_human Human No 5.7 IC50 = 1867 nM Funct
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
435 5 0 6 4.2 COc1ccc(-n2c(C(F)F)nnc2N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)cn1
CHEMBL4205046 v1ar_human Human No 7.7 IC50 = 19 nM Funct
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
408 2 1 4 4.9 Cc1ccn(C(=O)Nc2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1
CHEMBL106938 v1ar_human Human No 7.7 IC50 = 19 nM Bind
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V1a receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V1a receptor
594 7 2 4 5.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCC4)CC3)Cc3ccccc32)cc1
CHEMBL3938717 v1ar_human Human No 7.7 IC50 = 19 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
512 7 2 7 3.7 O=c1n(Cc2nnc(Cc3ccccc3Cl)[nH]2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F
CHEMBL3926829 v1ar_human Human No 7.7 IC50 = 19 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
579 10 3 7 2.9 O=CNC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(C(F)(F)F)c1
CHEMBL399289 v1ar_human Human No 7.7 IC50 = 19 nM Bind
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cells
548 5 2 4 6.1 COc1cc(C(=O)N2CCC3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl
CHEMBL70949 v1ar_rat Rat No 7.7 IC50 = 19 nM Bind
Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
433 3 2 3 6.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Nc3ccccc32)cc1
CHEMBL249536 v1ar_human Human No 6.7 IC50 = 190 nM Funct
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
532 4 1 4 6.2 COC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3Cl)cc1)c1ccccc1C2
CHEMBL59947 v1ar_rat Rat No 5.7 IC50 = 1900 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
334 2 0 2 3.3 O=C(c1ccccc1)N1CCC(N2C(=O)CCc3ccccc32)CC1
CHEMBL3353945 v1ar_human Human No 5.7 IC50 = 1900 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1055 20 11 14 -1.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccc2C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL118878 v1ar_rat Rat No 5.7 IC50 = 1900 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
428 4 2 4 4.6 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3N)cc2)c2ccccc21
CHEMBL118805 v1ar_rat Rat No 4.7 IC50 = 19000 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
441 4 0 3 5.3 Cc1ccccc1C(=O)N(C)c1ccc(C(=O)N2CCCC(N(C)C)c3ccccc32)cc1
CHEMBL119442 v1ar_rat Rat No 5.7 IC50 = 1910 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
386 4 1 3 4.5 COc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1
CHEMBL4542267 v1ar_human Human No 5.7 IC50 = 1979 nM Funct
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
485 7 0 8 3.5 COc1ccc(-n2c(CO[C@@H]3CCOC3)nnc2N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)cn1
CHEMBL1837013 v1ar_human Human No 6.7 IC50 = 199 nM Funct
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
333 3 0 5 3.7 Cc1ccccc1-n1c(C)nnc1C1CCN(c2ccccn2)CC1
CHEMBL3416885 v1ar_human Human Yes 8.7 IC50 = 2 nM Funct
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
437 4 0 4 4.5 CN(C)CCn1cc(C(=O)N2CCC3(CC2)OCc2ccccc23)c2ccc(Cl)cc21
CHEMBL389581 v1ar_human Human No 8.7 IC50 = 2 nM Bind
Binding affinity for human cloned vasopressin V1a receptor expressed in CHO cellsBinding affinity for human cloned vasopressin V1a receptor expressed in CHO cells
556 9 0 7 4.8 CC(C)(C)C(=O)C(C(=O)OCc1ccccc1)N1C(=O)[C@@H](N2C(=O)OC[C@@H]2c2ccccc2)[C@H]1/C=C/c1ccco1
CHEMBL1788220 v1ar_human Human No 8.7 IC50 = 2 nM Bind
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V1a receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V1a receptor
612 8 2 4 6.6 CN(C)CCNC(=O)C1=C[C@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL399888 v1ar_human Human No 8.7 IC50 = 2 nM Bind
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cells
612 8 2 4 6.6 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL71355 v1ar_rat Rat No 8.7 IC50 = 2 nM Bind
Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
485 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1Br
CHEMBL424663 v1ar_human Human No 8.7 IC50 = 2 nM Bind
Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor
378 2 0 2 5.7 Cc1ccc(-c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)cc1
CHEMBL4756737 v1ar_human Human No 8.7 IC50 = 2.2 nM Funct
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
382 2 0 5 5.1 Cc1cc([C@H]2CC[C@H](c3nnc4n3-c3ccc(Cl)cc3CCC4)CC2)no1
CHEMBL4756212 v1ar_human Human No 8.6 IC50 = 2.4 nM Funct
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
465 3 0 3 5.3 Cc1ccccc1N1CCN(C(=O)N2C[C@@H](C(=O)C3CCCC3)Cc3cc(Cl)ccc32)CC1
CHEMBL4778087 v1ar_human Human No 8.6 IC50 = 2.4 nM Funct
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
466 2 0 3 4.2 Cc1ccccc1N1CCN(C(=O)N2C[C@@H](C(=O)N3CCCC3)Cc3cc(Cl)ccc32)CC1
CHEMBL4759005 v1ar_human Human No 8.6 IC50 = 2.7 nM Funct
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
369 2 0 5 3.5 C#Cc1ccc2c(c1)CCCc1nnc(C3CCN(c4ccccn4)CC3)n1-2
CHEMBL603708 v1ar_human Human No 8.6 IC50 = 2.7 nM Funct
Antagonist activity at V1A receptor (unknown origin)Antagonist activity at V1A receptor (unknown origin)
446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL1834004 v1ar_human Human No 7.7 IC50 = 20 nM Funct
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
361 2 0 6 3.4 Cc1ccc2c(c1)COCc1nnc(C3CCN(c4ccccn4)CC3)n1-2
CHEMBL1837023 v1ar_human Human No 7.7 IC50 = 20 nM Funct
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
377 7 0 6 3.6 CCOCc1nnc(C2CCN(c3ccccn3)CC2)n1Cc1ccccc1
CHEMBL4781783 v1ar_human Human No 7.7 IC50 = 20 nM Funct
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
448 2 0 4 3.1 Cc1ccccc1N1CCN(C(=O)N2CN(S(C)(=O)=O)Cc3cc(Cl)ccc32)CC1
CHEMBL400266 v1ar_human Human No 7.7 IC50 = 20 nM Funct
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
542 5 2 3 7.0 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL68085 v1ar_human Human No 7.7 IC50 = 20 nM Bind
Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.
439 3 1 3 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1
CHEMBL101935 v1ar_human Human No 7.7 IC50 = 20 nM Bind
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptor
436 3 1 2 6.3 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1
CHEMBL68085 v1ar_rat Rat No 7.7 IC50 = 20 nM Bind
Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
439 3 1 3 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1
CHEMBL4741178 v1ar_human Human No 7.7 IC50 = 20 nM Funct
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
360 3 0 5 4.3 c1ccc(O[C@H]2CC[C@H](c3nnc4n3-c3ccccc3CCC4)CC2)nc1
CHEMBL1649949 v1ar_human Human Yes 6.7 IC50 = 200 nM Funct
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
311 3 0 3 4.9 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1
CHEMBL4760164 v1ar_human Human No 6.7 IC50 = 200 nM Funct
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
369 1 0 2 4.3 Cc1ccccc1N1CCN(C(=O)N2CCCc3cc(Cl)ccc32)CC1
CHEMBL61688 v1ar_rat Rat No 5.7 IC50 = 2000 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
379 3 0 4 3.2 O=C(c1ccc([N+](=O)[O-])cc1)N1CCC(N2C(=O)CCc3ccccc32)CC1
CHEMBL61947 v1ar_rat Rat No 5.7 IC50 = 2000 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
393 5 1 4 2.6 NCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL3353941 v1ar_human Human No 5.7 IC50 = 2000 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1033 19 11 14 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C2CCCCC2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL338294 v1ar_rat Rat No 5.7 IC50 = 2000 nM Bind
Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H]2CCCCN2C1=O
CHEMBL162588 v1ar_rat Rat No 5.7 IC50 = 2000 nM Bind
In vitro binding affinity for rat V1a receptorIn vitro binding affinity for rat V1a receptor
466 3 2 4 5.4 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1)c1ccc(F)cc1Cl
CHEMBL351587 v1ar_rat Rat No 5.7 IC50 = 2010 nM Bind
In vitro binding affinity for rat V1a receptorIn vitro binding affinity for rat V1a receptor
442 3 1 5 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3cn(C)nc3-c3sccc32)cc1
CHEMBL420500 v1ar_human Human Yes 5.7 IC50 = 2010 nM Bind
Inhibition of human V1A vasopressin receptorInhibition of human V1A vasopressin receptor
409 3 1 6 2.5 O=C(OCc1ccc2c(c1)OCO2)N1CCC2(CC1)C(=O)NCN2c1ccccc1
CHEMBL128688 v1ar_human Human No 5.7 IC50 = 2010 nM Funct
Inhibition of vasopressin induced calcium immobilization in human V1a receptor expressing cellsInhibition of vasopressin induced calcium immobilization in human V1a receptor expressing cells
536 7 2 4 7.0 O=C(O)CC[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1
CHEMBL4746818 v1ar_human Human No 7.7 IC50 = 21 nM Funct
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
479 3 0 3 5.0 Cc1ccccc1N1CCN(C(=O)C2CN(C(=O)C3CCCCC3)Cc3cc(Cl)ccc32)CC1
CHEMBL297990 v1ar_rat Rat No 7.7 IC50 = 21 nM Bind
In vitro inhibition of (Phe-3,4,5 [3H]-) AVP binding towards isolated rat hepatic Vasopressin V1a receptorIn vitro inhibition of (Phe-3,4,5 [3H]-) AVP binding towards isolated rat hepatic Vasopressin V1a receptor
422 3 1 4 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1
CHEMBL194970 v1ar_human Human No 7.7 IC50 = 21 nM Bind
Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor
442 3 0 4 4.8 Cc1ccc(S(=O)(=O)c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)cc1
CHEMBL60096 v1ar_rat Rat No 6.7 IC50 = 210 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
463 8 1 4 3.6 CC(=O)NCCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL60736 v1ar_rat Rat No 6.7 IC50 = 210 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
378 4 0 3 3.7 CCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL3354600 v1ar_human Human No 5.7 IC50 = 2100 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1029 20 11 14 -1.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccs2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL349506 v1ar_rat Rat No 5.7 IC50 = 2100 nM Bind
In vitro binding affinity for rat V1a receptorIn vitro binding affinity for rat V1a receptor
496 3 1 5 5.9 Cn1cc2c(n1)-c1sccc1N(C(=O)c1ccc(NC(=O)c3ccc(Cl)cc3Cl)cc1)CC2
CHEMBL350383 v1ar_rat Rat No 5.7 IC50 = 2100 nM Bind
In vitro binding affinity for rat V1a receptorIn vitro binding affinity for rat V1a receptor
428 3 2 4 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1
CHEMBL341173 v1ar_human Human No 5.7 IC50 = 2130 nM Funct
Inhibition of vasopressin induced calcium immobilization in human V1a receptor expressing cellsInhibition of vasopressin induced calcium immobilization in human V1a receptor expressing cells
522 6 2 4 6.6 O=C(O)C[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1
CHEMBL2112895 v1ar_rat Rat No 6.7 IC50 = 220 nM Bind
Displacement of [3H]AVP from binding to arginine vasopressin 1a (V1a) column of rat liverDisplacement of [3H]AVP from binding to arginine vasopressin 1a (V1a) column of rat liver
637 11 3 8 1.9 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)NC2CCNCC2)C3(C)C)CC1
CHEMBL4756354 v1ar_human Human No 6.7 IC50 = 220 nM Funct
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
452 5 0 7 4.6 COC(=O)CC1Cc2cc(Cl)ccc2-n2c1nnc2[C@H]1CC[C@H](Oc2ccccn2)CC1
CHEMBL4204210 v1ar_human Human Yes 5.7 IC50 = 2200 nM Funct
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
531 4 2 6 4.2 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N(C)C
CHEMBL3353950 v1ar_human Human No 5.7 IC50 = 2200 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1042 20 11 15 -2.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccn2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL119534 v1ar_rat Rat No 5.7 IC50 = 2200 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
386 4 1 3 4.5 COc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)cc1
CHEMBL115444 v1ar_human Human No 5.7 IC50 = 2220 nM Bind
Inhibition of human V1A vasopressin receptorInhibition of human V1A vasopressin receptor
429 3 1 7 4.1 O=C(OCc1cc2c(cc1Cl)OCO2)N1CCC(n2c(O)nc3ccccc32)CC1
CHEMBL316736 v1ar_human Human No 6.6 IC50 = 227 nM Funct
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
596 7 2 5 4.8 O=C(NCCN1CCOCC1)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2
CHEMBL3975038 v1ar_human Human No 7.6 IC50 = 23 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
548 7 1 7 5.4 O=c1n(Cc2nnc(Cc3ccccc3C(F)(F)F)[nH]2)nc(-c2ccc(Cl)s2)n1Cc1ccccc1F
CHEMBL418890 v1ar_rat Rat No 7.6 IC50 = 23 nM Bind
Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.
475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl
CHEMBL418890 v1ar_rat Rat No 7.6 IC50 = 23 nM Bind
In vitro binding affinity for rat V1a receptorIn vitro binding affinity for rat V1a receptor
475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl
CHEMBL418890 v1ar_rat Rat No 7.6 IC50 = 23 nM Bind
Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl
CHEMBL3947893 v1ar_human Human No 6.6 IC50 = 230 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
532 6 1 7 5.3 O=c1n(Cc2cnc(-c3cccc(Cl)c3Cl)o2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F
CHEMBL49429 v1ar_human Human Yes 6.6 IC50 = 230 nM Bind
Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL159831 v1ar_rat Rat No 6.6 IC50 = 230 nM Bind
In vitro binding affinity for rat V1a receptorIn vitro binding affinity for rat V1a receptor
478 3 1 3 6.9 O=C(Nc1ccc(C(=O)N2CCCCc3sc(Cl)cc32)cc1)c1ccc(Cl)cc1Cl
CHEMBL49429 v1ar_human Human Yes 6.6 IC50 = 230 nM Bind
In vitro binding affinity to human V1a receptorIn vitro binding affinity to human V1a receptor
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL49429 v1ar_human Human Yes 6.6 IC50 = 230 nM Bind
In vitro inhibition of [3H]- AVP binding to V1a receptor from human platelet membraneIn vitro inhibition of [3H]- AVP binding to V1a receptor from human platelet membrane
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL118204 v1ar_rat Rat No 5.6 IC50 = 2300 nM Bind
Compound was tested for its ability to displace [3H]AVP from its specific binding sites in Rat liver (AVP-V1a receptor).Compound was tested for its ability to displace [3H]AVP from its specific binding sites in Rat liver (AVP-V1a receptor).
455 4 1 5 5.0 CC(=O)O/N=C1\CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21
CHEMBL332757 v1ar_rat Rat No 5.6 IC50 = 2300 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
384 5 1 2 4.9 O=C(CCc1ccccc1)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1
CHEMBL2112899 v1ar_rat Rat No 5.6 IC50 = 2300 nM Bind
Displacement of [3H]AVP from binding to arginine vasopressin 1a (V1a) column of rat liverDisplacement of [3H]AVP from binding to arginine vasopressin 1a (V1a) column of rat liver
530 8 3 5 2.2 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@@H](N)CCC(N)=O)C2
CHEMBL281361 v1ar_rat Rat No 5.6 IC50 = 2300 nM Bind
Inhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptorInhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptor
589 7 1 5 4.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@H](NCc3ccccc3)C1=O)C2
CHEMBL1837015 v1ar_human Human No 5.6 IC50 = 2310 nM Funct
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
344 3 0 6 3.2 Cc1nnc(C2CCN(c3ccccn3)CC2)n1-c1ccc(C#N)cc1
CHEMBL280202 v1ar_rat Rat No 5.6 IC50 = 2340 nM Bind
Inhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptorInhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptor
555 7 0 5 4.0 CCN(CC)[C@@H]1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O
CHEMBL419183 v1ar_human Human No 7.6 IC50 = 24 nM Bind
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V1a receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V1a receptor
599 7 3 4 6.1 O=C(O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL3909988 v1ar_human Human No 7.6 IC50 = 24 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
637 11 3 8 4.0 CCNC(=O)OCC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(C(F)(F)F)c1
CHEMBL430841 v1ar_human Human No 7.6 IC50 = 24 nM Bind
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V1a receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V1a receptor
561 4 1 3 7.6 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(C5)N4Cc4cc(Cl)ccc43)cc2)cc1
CHEMBL443498 v1ar_human Human No 7.6 IC50 = 24 nM Bind
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V1a receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V1a receptor
547 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1
CHEMBL60672 v1ar_rat Rat No 6.6 IC50 = 240 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
435 8 1 4 2.8 O=CNCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL350383 v1ar_human Human No 6.6 IC50 = 240 nM Bind
In vitro binding affinity to human V1a receptorIn vitro binding affinity to human V1a receptor
428 3 2 4 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1
CHEMBL304956 v1ar_rat Rat No 6.6 IC50 = 240 nM Bind
Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
435 3 1 3 5.6 Cc1cccc(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)c1C
CHEMBL324935 v1ar_rat Rat Yes 5.6 IC50 = 2400 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
322 3 1 2 3.9 CC(C)C(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1
CHEMBL331098 v1ar_rat Rat No 5.6 IC50 = 2400 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
427 4 1 3 5.3 Cc1cccc(C(=O)Nc2ccc(C(=O)N3CCCC(N(C)C)c4ccccc43)cc2)c1
CHEMBL1837026 v1ar_human Human No 5.6 IC50 = 2460 nM Funct
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
407 8 1 7 2.7 O=C(O)COCc1nnc(C2CCN(c3ccccn3)CC2)n1Cc1ccccc1
CHEMBL1837024 v1ar_human Human No 7.6 IC50 = 25 nM Funct
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
418 6 0 7 2.9 c1ccc(Cn2c(CN3CCOCC3)nnc2C2CCN(c3ccccn3)CC2)cc1
CHEMBL4790089 v1ar_human Human No 7.6 IC50 = 25 nM Funct
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
465 3 0 3 5.3 Cc1ccccc1N1CCN(C(=O)N2C[C@H](C(=O)C3CCCC3)Cc3cc(Cl)ccc32)CC1
CHEMBL3923775 v1ar_human Human No 7.6 IC50 = 25 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
607 9 3 7 3.5 CC(=O)NC(C)(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(C(F)(F)F)c1
CHEMBL81755 v1ar_human Human No 7.6 IC50 = 25 nM Bind
Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.
473 3 1 3 6.1 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1Cl
CHEMBL4786172 v1ar_human Human No 7.6 IC50 = 25 nM Funct
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
348 2 0 5 4.5 Cc1cc([C@H]2CC[C@H](c3nnc4n3-c3ccccc3CCC4)CC2)no1
CHEMBL59699 v1ar_rat Rat No 6.6 IC50 = 250 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
449 9 1 4 3.2 O=CNCCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL106229 v1ar_human Human No 6.6 IC50 = 250 nM Bind
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V1a receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V1a receptor
385 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCNc3ccccc32)cc1
CHEMBL304430 v1ar_rat Rat No 5.6 IC50 = 2500 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
340 2 0 3 3.3 O=C(c1cccs1)N1CCC(N2C(=O)CCc3ccccc32)CC1
CHEMBL3354578 v1ar_human Human No 5.6 IC50 = 2500 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
975 21 10 13 -3.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CCOC)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL118244 v1ar_rat Rat Yes 5.6 IC50 = 2500 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
406 4 1 3 4.5 O=C(c1ccc(NS(=O)(=O)c2ccccc2)cc1)N1CCCCc2ccccc21
CHEMBL303376 v1ar_rat Rat No 5.6 IC50 = 2500 nM Bind
Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
432 3 1 2 6.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2c3ccccc3CCc3ccccc32)cc1
CHEMBL4797387 v1ar_human Human No 6.6 IC50 = 252 nM Funct
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
373 3 0 5 4.1 CCc1ccc2c(c1)CCCc1nnc(C3CCN(c4ccccn4)CC3)n1-2
CHEMBL411 v1ar_human Human Yes 4.6 IC50 = 25925 nM Bind
DRUGMATRIX: Vasopressin V1A radioligand binding (ligand: [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr)DRUGMATRIX: Vasopressin V1A radioligand binding (ligand: [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr)
268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1
CHEMBL70981 v1ar_rat Rat No 7.6 IC50 = 26 nM Bind
Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.
439 3 1 3 5.4 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1
CHEMBL71305 v1ar_rat Rat No 7.6 IC50 = 26 nM Bind
Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.
475 3 1 3 6.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1C(F)(F)F
CHEMBL101678 v1ar_human Human No 7.6 IC50 = 26 nM Bind
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptor
512 4 1 2 7.9 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL70981 v1ar_rat Rat No 7.6 IC50 = 26 nM Bind
Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
439 3 1 3 5.4 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1
CHEMBL71305 v1ar_rat Rat No 7.6 IC50 = 26 nM Bind
Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
475 3 1 3 6.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1C(F)(F)F
CHEMBL4760698 v1ar_human Human No 6.6 IC50 = 260 nM Funct
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
370 2 0 4 3.4 CN1CCN(C(=O)C2CCN(c3ccccn3)CC2)c2ccc(Cl)cc21
CHEMBL3917760 v1ar_human Human No 6.6 IC50 = 260 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
508 6 1 6 5.1 O=c1n(Cc2cncc(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1CC(O)C(F)(F)F
CHEMBL3965329 v1ar_human Human No 6.6 IC50 = 260 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
547 6 1 6 6.4 O=c1n(Cc2ccc(-c3cccc(Cl)c3Cl)s2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F
CHEMBL296619 v1ar_rat Rat No 6.6 IC50 = 260 nM Bind
Displacement of (Phe-3,4,5 [3H]-) AVP from isolated rat hepatic V1a receptorDisplacement of (Phe-3,4,5 [3H]-) AVP from isolated rat hepatic V1a receptor
519 4 1 5 6.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(-c2ccccn2)ccc1Cl
CHEMBL4751140 v1ar_human Human No 6.6 IC50 = 260 nM Funct
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
356 2 1 4 3.4 O=C(C1CCN(c2ccccn2)CC1)N1CCNc2cc(Cl)ccc21
CHEMBL2112249 v1ar_rat Rat No 5.6 IC50 = 2600 nM Bind
Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O
CHEMBL119318 v1ar_rat Rat No 5.6 IC50 = 2600 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
481 4 1 3 6.3 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3cc(Cl)cc(Cl)c3)cc2)c2ccccc21
CHEMBL333597 v1ar_rat Rat No 5.6 IC50 = 2600 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
458 5 1 5 4.9 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3[N+](=O)[O-])cc2)c2ccccc21
CHEMBL64319 v1ar_rat Rat No 4.6 IC50 = 26000 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
336 2 0 4 2.1 O=C(c1cnccn1)N1CCC(N2C(=O)CCc3ccccc32)CC1
CHEMBL115853 v1ar_rat Rat No 4.6 IC50 = 26000 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
427 4 1 3 5.3 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCC(N(C)C)c4ccccc43)cc2)cc1
CHEMBL429281 v1ar_human Human No 6.6 IC50 = 262 nM Bind
Binding affinity for human cloned vasopressin V1a receptor expressed in CHO cellsBinding affinity for human cloned vasopressin V1a receptor expressed in CHO cells
571 10 1 4 5.9 CC(C)C[C@@H](C(=O)NCc1ccc(Cl)cc1)N1C(=O)[C@@H](N2C(=O)OC[C@@H]2c2ccccc2)[C@H]1/C=C/c1ccccc1
CHEMBL249740 v1ar_human Human No 7.6 IC50 = 27 nM Funct
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
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
CHEMBL3911148 v1ar_human Human No 7.6 IC50 = 27 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
498 6 1 8 3.6 O=c1n(Cc2cn(-c3ccccc3Cl)nn2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F
CHEMBL71282 v1ar_rat Rat No 7.6 IC50 = 27 nM Bind
Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1cccc(Cl)c1Cl
CHEMBL3353953 v1ar_human Human No 6.6 IC50 = 270 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1055 21 11 14 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCc2ccccc2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL303176 v1ar_rat Rat No 6.6 IC50 = 270 nM Bind
Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
421 3 1 3 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3cccn3-c3ccccc32)cc1
CHEMBL333055 v1ar_rat Rat No 5.6 IC50 = 2700 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
401 4 1 4 4.4 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccccc1[N+](=O)[O-]
CHEMBL1837036 v1ar_human Human No 6.6 IC50 = 272 nM Funct
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
360 2 0 6 3.0 CN1Cc2ccccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1
CHEMBL429971 v1ar_rat Rat No 5.6 IC50 = 2750 nM Bind
Inhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptorInhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptor
542 7 2 6 2.2 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(NCCN)C1=O)C2
CHEMBL418692 v1ar_rat Rat No 6.6 IC50 = 280 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
435 8 1 4 3.8 NCCCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL4746818 v1ar_human Human No 6.6 IC50 = 280 nM Funct
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
479 3 0 3 5.0 Cc1ccccc1N1CCN(C(=O)C2CN(C(=O)C3CCCCC3)Cc3cc(Cl)ccc32)CC1
CHEMBL4785083 v1ar_human Human No 6.6 IC50 = 280 nM Funct
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
383 0 1 3 4.2 O=C(N1CCC2(CC1)OCc1ccccc12)N1CCNc2cc(Cl)ccc21
CHEMBL3354571 v1ar_human Human No 6.6 IC50 = 280 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1061 21 11 15 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCc2cccs2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL198446 v1ar_human Human No 6.6 IC50 = 280 nM Bind
Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor
394 3 0 3 5.8 Cc1ccc(Oc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)cc1
CHEMBL302233 v1ar_rat Rat No 5.6 IC50 = 2800 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
391 3 1 3 3.2 CC(=O)Nc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL4764410 v1ar_human Human No 5.6 IC50 = 2800 nM Funct
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
336 1 1 3 3.2 Cc1ccccc1N1CCN(C(=O)N2CCNc3ccccc32)CC1
CHEMBL118562 v1ar_rat Rat No 5.6 IC50 = 2800 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
386 4 1 3 4.5 COc1cccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)c1
CHEMBL119671 v1ar_rat Rat No 5.6 IC50 = 2800 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
487 4 1 3 6.6 O=C(Nc1ccc(C(=O)N2CCCC(N3CCCCC3)c3ccccc32)cc1)c1ccccc1Cl
CHEMBL120449 v1ar_rat Rat No 5.6 IC50 = 2800 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
456 4 3 3 4.7 CNC(=O)NC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21
CHEMBL4591825 v1ar_human Human Yes 5.5 IC50 = 2885 nM Funct
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
429 6 0 7 3.4 COCc1nnc(N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1
CHEMBL1837020 v1ar_human Human No 7.5 IC50 = 29 nM Funct
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
367 4 0 5 4.1 Cc1nnc(C2CCN(c3ccccn3)CC2)n1Cc1cccc(Cl)c1
CHEMBL3943019 v1ar_human Human No 7.5 IC50 = 29 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
514 6 1 7 5.1 O=c1n(Cc2ncc(-c3ccccc3Cl)s2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F
CHEMBL106938 v1ar_human Human No 7.5 IC50 = 29 nM Funct
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
594 7 2 4 5.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCC4)CC3)Cc3ccccc32)cc1
CHEMBL321656 v1ar_human Human No 7.5 IC50 = 29 nM Funct
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
626 9 2 4 7.0 CN(C)CCCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL324251 v1ar_rat Rat No 6.5 IC50 = 290 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
470 6 2 4 4.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)CC(N)=O)c3ccccc32)cc1
CHEMBL279022 v1ar_rat Rat No 5.5 IC50 = 2900 nM Bind
Inhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptorInhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptor
589 7 1 5 4.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](NCc3ccccc3)C1=O)C2
CHEMBL283317 v1ar_rat Rat No 5.5 IC50 = 2970 nM Bind
Inhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptorInhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptor
555 7 0 5 4.0 CCN(CC)[C@H]1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O
CHEMBL1837028 v1ar_human Human No 8.5 IC50 = 3 nM Funct
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
434 6 0 8 3.4 Clc1cccc(Cn2c(Cn3nccn3)nnc2C2CCN(c3ccccn3)CC2)c1
CHEMBL4297183 v1ar_human Human No 8.5 IC50 = 3 nM Funct
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
409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1
CHEMBL1755 v1ar_human Human Yes 8.5 IC50 = 3 nM Funct
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
498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1
CHEMBL4297183 v1ar_human Human No 8.5 IC50 = 3 nM Funct
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
409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1
CHEMBL381248 v1ar_human Human No 8.5 IC50 = 3 nM Bind
Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor
364 2 0 2 5.4 O=C(c1ccc(-c2ccccc2)cc1)N1Cc2cccn2Cc2ccccc21
CHEMBL1837038 v1ar_human Human No 8.5 IC50 = 3.2 nM Funct
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
438 2 0 7 3.8 COC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1
CHEMBL4778839 v1ar_human Human No 8.5 IC50 = 3.2 nM Funct
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
379 2 0 5 4.2 Clc1ccc2c(c1)CCCc1nnc(C3CCN(c4ccccn4)CC3)n1-2
CHEMBL159823 v1ar_rat Rat No 8.5 IC50 = 3.4 nM Bind
In vitro binding affinity for rat V1a receptorIn vitro binding affinity for rat V1a receptor
483 4 1 3 6.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1
CHEMBL519240 v1ar_human Human Yes 8.4 IC50 = 3.9 nM Bind
Displacement of radiolabeled [d(CH2)51,Tyr(Me)2]-AVP from human vasopressin V1a receptorDisplacement of radiolabeled [d(CH2)51,Tyr(Me)2]-AVP from human vasopressin V1a receptor
327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1
CHEMBL297705 v1ar_rat Rat No 7.5 IC50 = 30 nM Bind
Displacement of (Phe-3,4,5 [3H]-) AVP from isolated rat hepatic V1a receptorDisplacement of (Phe-3,4,5 [3H]-) AVP from isolated rat hepatic V1a receptor
484 4 1 4 6.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1-c1ccccc1
CHEMBL102311 v1ar_human Human No 7.5 IC50 = 30 nM Bind
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptor
466 4 1 3 6.3 COc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1
CHEMBL59754 v1ar_rat Rat No 6.5 IC50 = 300 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
519 12 1 4 5.1 CC(=O)NCCCCCCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL4794001 v1ar_human Human No 6.5 IC50 = 300 nM Funct
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
384 1 0 3 3.8 Cc1ccccc1N1CCN(C(=O)N2CCN(C)c3cc(Cl)ccc32)CC1
CHEMBL3354583 v1ar_human Human No 6.5 IC50 = 300 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
974 21 10 12 -1.9 CCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1
CHEMBL338020 v1ar_rat Rat No 5.5 IC50 = 3000 nM Bind
Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.
None None None CC(C)C[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O
CHEMBL118270 v1ar_rat Rat No 5.5 IC50 = 3000 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
447 4 1 3 5.6 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3Cl)cc2)c2ccccc21
CHEMBL334225 v1ar_rat Rat No 5.5 IC50 = 3000 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
413 4 1 3 5.0 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3)cc2)c2ccccc21
CHEMBL3925572 v1ar_human Human No 7.5 IC50 = 31 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
497 6 1 7 4.2 O=c1n(Cc2cnn(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F
CHEMBL304956 v1ar_rat Rat No 7.5 IC50 = 31 nM Bind
Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.
435 3 1 3 5.6 Cc1cccc(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)c1C
CHEMBL73286 v1ar_rat Rat No 7.5 IC50 = 31 nM Bind
Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.
437 4 1 4 5.0 COc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1
CHEMBL73286 v1ar_rat Rat No 7.5 IC50 = 31 nM Bind
Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
437 4 1 4 5.0 COc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1
CHEMBL49657 v1ar_rat Rat No 6.5 IC50 = 310 nM Bind
Displacement of (Phe-3,4,5 [3H]-) AVP from isolated rat hepatic V1a receptorDisplacement of (Phe-3,4,5 [3H]-) AVP from isolated rat hepatic V1a receptor
444 3 1 4 4.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(F)ccc1F
CHEMBL293922 v1ar_rat Rat No 5.5 IC50 = 3100 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
359 2 0 3 3.1 N#Cc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL60726 v1ar_rat Rat No 5.5 IC50 = 3100 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
379 3 0 4 3.2 O=C(c1cccc([N+](=O)[O-])c1)N1CCC(N2C(=O)CCc3ccccc32)CC1
CHEMBL165670 v1ar_human Human No 5.5 IC50 = 3100 nM Bind
Binding affinity towards VIa receptorBinding affinity towards VIa receptor
471 4 2 2 6.7 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1
CHEMBL118220 v1ar_rat Rat No 5.5 IC50 = 3100 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
370 3 1 2 4.8 Cc1cccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)c1
CHEMBL334777 v1ar_human Human No 6.5 IC50 = 314 nM Bind
Ability to displace [3H]arginine vasopressin in cloned human V1a receptorAbility to displace [3H]arginine vasopressin in cloned human V1a receptor
536 7 2 4 7.0 O=C(O)CC[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1
CHEMBL81269 v1ar_human Human No 7.5 IC50 = 32 nM Bind
Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.
505 4 1 4 6.3 COc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1NC(=O)c1ccc(Cl)cc1Cl
CHEMBL399288 v1ar_human Human No 7.5 IC50 = 32 nM Bind
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cells
518 4 2 3 6.1 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3Cl)cc1)c1ccccc1C2
CHEMBL59740 v1ar_rat Rat No 6.5 IC50 = 320 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
392 5 0 3 4.1 CCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL400860 v1ar_human Human No 6.5 IC50 = 320 nM Funct
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
572 5 2 5 6.0 COc1cc(C(=O)N2CC[C@]3(C=C(C4=NCCN4)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl
CHEMBL2112898 v1ar_rat Rat No 6.5 IC50 = 320 nM Bind
Displacement of [3H]AVP from binding to arginine vasopressin 1a (V1a) column of rat liverDisplacement of [3H]AVP from binding to arginine vasopressin 1a (V1a) column of rat liver
568 10 2 7 1.8 CN[C@@H](CCS(C)(=O)=O)C(=O)N[C@H]1CC2CC[C@]1(CS(=O)(=O)N1CCN(c3ccccc3C)CC1)C2(C)C
CHEMBL2391300 v1ar_rat Rat No 6.5 IC50 = 320 nM Bind
Inhibition of rat liver V1a receptorInhibition of rat liver V1a receptor
568 10 2 7 1.8 CN[C@@H](CCS(C)(=O)=O)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccccc3C)CC1)C2(C)C
CHEMBL3353952 v1ar_human Human No 5.5 IC50 = 3200 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1042 20 11 15 -2.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccncc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL339118 v1ar_rat Rat No 5.5 IC50 = 3200 nM Bind
Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O
CHEMBL119591 v1ar_rat Rat No 5.5 IC50 = 3200 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
441 4 2 3 4.9 CC(=O)NC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21
CHEMBL119730 v1ar_rat Rat No 5.5 IC50 = 3200 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
370 4 1 2 4.5 O=C(Cc1ccccc1)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1
CHEMBL323802 v1ar_rat Rat No 5.5 IC50 = 3200 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
452 5 1 4 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)CC#N)c3ccccc32)cc1
CHEMBL435021 v1ar_rat Rat No 4.5 IC50 = 32000 nM Bind
Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CNCCN2C(=O)[C@H]2CCCCN2C1=O
CHEMBL300946 v1ar_rat Rat Yes 7.5 IC50 = 33 nM Bind
Displacement of (Phe-3,4,5 [3H]-) AVP from isolated rat hepatic V1a receptorDisplacement of (Phe-3,4,5 [3H]-) AVP from isolated rat hepatic V1a receptor
440 3 1 4 4.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1
CHEMBL310581 v1ar_rat Rat No 7.5 IC50 = 33 nM Bind
Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.
471 4 1 4 5.6 COc1cc(Cl)ccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1
CHEMBL82376 v1ar_rat Rat No 7.5 IC50 = 33 nM Bind
Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.
489 3 1 3 6.6 Cc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1NC(=O)c1ccc(Cl)cc1Cl
CHEMBL1788220 v1ar_rat Rat No 7.5 IC50 = 33 nM Bind
Evaluated for binding affinity towards vasopressin V1a receptor in ratEvaluated for binding affinity towards vasopressin V1a receptor in rat
612 8 2 4 6.6 CN(C)CCNC(=O)C1=C[C@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL293863 v1ar_rat Rat No 6.5 IC50 = 330 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
376 4 0 2 4.2 CCCc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL304485 v1ar_rat Rat No 6.5 IC50 = 330 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
421 7 1 4 3.4 NCCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL3354599 v1ar_human Human No 6.5 IC50 = 330 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1022 21 10 12 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CCc2ccccc2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL52813 v1ar_rat Rat No 5.5 IC50 = 3300 nM Bind
Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O
CHEMBL117566 v1ar_rat Rat No 5.5 IC50 = 3300 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
384 3 1 2 5.1 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)c(C)c1
CHEMBL3965167 v1ar_human Human No 7.5 IC50 = 34 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
496 7 2 7 3.2 O=c1n(Cc2nnc(Cc3ccccc3F)[nH]2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F
CHEMBL49429 v1ar_rat Rat Yes 6.5 IC50 = 340 nM Bind
Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL420216 v1ar_human Human No 6.5 IC50 = 340 nM Bind
Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.
469 3 1 3 6.2 Cc1ccc(C)c(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)c1
CHEMBL49429 v1ar_rat Rat Yes 6.5 IC50 = 340 nM Bind
In vitro binding affinity for rat V1a receptorIn vitro binding affinity for rat V1a receptor
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL3353943 v1ar_human Human No 5.5 IC50 = 3400 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1009 21 12 15 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCCO)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL1837011 v1ar_human Human No 6.5 IC50 = 345 nM Funct
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
319 3 0 5 3.4 Cc1nnc(C2CCN(c3ccccn3)CC2)n1-c1ccccc1
CHEMBL1837029 v1ar_human Human No 6.5 IC50 = 345 nM Funct
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
347 2 0 6 3.1 c1ccc(N2CCC(c3nnc4n3-c3ccccc3COC4)CC2)nc1
CHEMBL4744606 v1ar_human Human No 7.5 IC50 = 35 nM Funct
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
428 2 1 4 2.7 Cc1ccccc1N1CCN(C(=O)N2CN(C(=O)CO)Cc3cc(Cl)ccc32)CC1
CHEMBL4753130 v1ar_human Human No 7.5 IC50 = 35 nM Funct
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
465 3 0 3 4.6 Cc1ccccc1N1CCN(C(=O)C2CN(C(=O)C3CCCC3)Cc3cc(Cl)ccc32)CC1
CHEMBL4758331 v1ar_human Human No 7.5 IC50 = 35 nM Funct
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
474 2 0 3 5.0 Cc1ccccc1N1CCN(C(=O)N2CN(C(=O)c3ccccc3)Cc3cc(Cl)ccc32)CC1
CHEMBL4127791 v1ar_human Human No 7.5 IC50 = 35 nM Funct
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
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
CHEMBL318392 v1ar_human Human No 7.5 IC50 = 35 nM Bind
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V1a receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V1a receptor
519 3 1 3 6.6 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(CC4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1Cl
CHEMBL321561 v1ar_human Human No 7.5 IC50 = 35 nM Bind
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V1a receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V1a receptor
595 4 1 3 8.2 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(C5)N4Cc4cc(Cl)ccc43)c(Cl)c2)cc1
CHEMBL59900 v1ar_rat Rat No 6.5 IC50 = 350 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
390 5 0 2 4.6 CCCCc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL3353955 v1ar_human Human No 6.5 IC50 = 350 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1056 21 11 15 -2.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCc2ccncc2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL62344 v1ar_rat Rat No 5.5 IC50 = 3500 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
392 3 0 4 3.1 COC(=O)c1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL2370623 v1ar_rat Rat No 5.5 IC50 = 3500 nM Bind
Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCC=NN2C1=O
CHEMBL295014 v1ar_human Human No 7.4 IC50 = 36 nM Bind
In vitro inhibition of [3H]- AVP binding to V1a receptor from human platelet membraneIn vitro inhibition of [3H]- AVP binding to V1a receptor from human platelet membrane
438 3 1 3 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccsc3Cc3ccccc32)cc1
CHEMBL61154 v1ar_rat Rat No 6.4 IC50 = 360 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
465 7 1 5 3.4 COC(=O)NCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL2112896 v1ar_rat Rat No 6.4 IC50 = 360 nM Bind
Displacement of [3H]AVP from binding to arginine vasopressin 1a (V1a) column of rat liverDisplacement of [3H]AVP from binding to arginine vasopressin 1a (V1a) column of rat liver
582 10 1 7 2.1 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)N(C)C)C3(C)C)CC1
CHEMBL116463 v1ar_human Human No 5.4 IC50 = 3650 nM Bind
Inhibition of human V1A vasopressin receptorInhibition of human V1A vasopressin receptor
517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1
CHEMBL420031 v1ar_human Human No 7.4 IC50 = 37 nM Bind
Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.
493 3 1 3 6.4 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccc(F)cc1Cl
CHEMBL400266 v1ar_human Human No 7.4 IC50 = 37 nM Bind
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cells
542 5 2 3 7.0 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL1774024 v1ar_human Human No 7.4 IC50 = 37.2 nM Funct
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
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
CHEMBL2112903 v1ar_rat Rat No 6.4 IC50 = 370 nM Bind
Displacement of [3H]AVP from binding to arginine vasopressin 1a (V1a) column of rat liverDisplacement of [3H]AVP from binding to arginine vasopressin 1a (V1a) column of rat liver
554 9 2 7 1.5 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@@H](N)CCS(C)(=O)=O)C3(C)C)CC1
CHEMBL159359 v1ar_human Human No 6.4 IC50 = 370 nM Bind
In vitro binding affinity to human V1a receptorIn vitro binding affinity to human V1a receptor
517 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1
CHEMBL1253853 v1ar_rat Rat Yes 6.4 IC50 = 370 nM Bind
Inhibition of rat liver V1a receptorInhibition of rat liver V1a receptor
554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C
CHEMBL64520 v1ar_rat Rat No 5.4 IC50 = 3700 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
349 2 1 3 2.9 Nc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL64836 v1ar_rat Rat No 5.4 IC50 = 3700 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
392 3 0 4 3.2 CC(=O)Oc1cccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)c1
CHEMBL2112247 v1ar_rat Rat No 5.4 IC50 = 3700 nM Bind
Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O
CHEMBL416505 v1ar_rat Rat No 4.4 IC50 = 37000 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
335 2 0 3 2.7 O=C(c1ccncc1)N1CCC(N2C(=O)CCc3ccccc32)CC1
CHEMBL249741 v1ar_human Human Yes 7.4 IC50 = 38 nM Funct
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
548 5 2 4 6.1 COc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl
CHEMBL71797 v1ar_rat Rat No 7.4 IC50 = 38 nM Bind
Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.
421 3 1 3 5.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1
CHEMBL71797 v1ar_rat Rat No 7.4 IC50 = 38 nM Bind
Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
421 3 1 3 5.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1
CHEMBL4776471 v1ar_human Human No 6.4 IC50 = 380 nM Funct
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
369 1 1 2 4.9 Cc1ccccc1C1CCN(C(=O)N2CCNc3cc(Cl)ccc32)CC1
CHEMBL3354601 v1ar_human Human No 6.4 IC50 = 380 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1029 20 11 14 -1.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccs2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL249340 v1ar_human Human No 6.4 IC50 = 380 nM Funct
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
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
CHEMBL332685 v1ar_rat Rat No 6.4 IC50 = 380 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
399 3 1 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(C)c3ccccc32)cc1
CHEMBL4564411 v1ar_human Human No 5.4 IC50 = 3811 nM Funct
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
429 6 0 7 3.4 COCc1nnc(N2C[C@@H]3C[C@]3(c3cccc(F)c3Cl)C2)n1-c1ccc(OC)nc1
CHEMBL242517 v1ar_human Human No 7.4 IC50 = 39 nM Bind
Binding affinity for human cloned vasopressin V1a receptor expressed in CHO cellsBinding affinity for human cloned vasopressin V1a receptor expressed in CHO cells
538 10 0 5 5.6 CC(C)C[C@@H](C(=O)OCc1ccccc1)N1C(=O)[C@@H](N2C(=O)OC[C@@H]2c2ccccc2)[C@H]1/C=C/c1ccccc1
CHEMBL3943296 v1ar_human Human No 7.4 IC50 = 39 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
596 7 1 10 3.2 O=c1n(S(=O)(=O)c2ncnn2Cc2ccccc2C(F)(F)F)nc(-c2ccc(Cl)cc2)n1CC(O)C(F)(F)F
CHEMBL4749660 v1ar_human Human No 6.4 IC50 = 390 nM Funct
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
383 1 0 2 4.7 Cc1ccccc1N1CCN(C(=O)N2CCCCc3cc(Cl)ccc32)CC1
CHEMBL3354570 v1ar_human Human No 6.4 IC50 = 390 nM Bind
Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAntagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
1031 20 11 15 -1.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccco2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O
CHEMBL420880 v1ar_rat Rat No 6.4 IC50 = 390 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
399 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N)c3ccccc32)cc1
CHEMBL109166 v1ar_human Human No 8.4 IC50 = 4 nM Bind
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V1a receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V1a receptor
527 6 3 4 4.5 O=C(NCCO)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2
CHEMBL1788221 v1ar_human Human No 8.4 IC50 = 4 nM Bind
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V1a receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V1a receptor
554 7 2 4 5.1 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2
CHEMBL316736 v1ar_human Human No 8.4 IC50 = 4 nM Bind
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V1a receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V1a receptor
596 7 2 5 4.8 O=C(NCCN1CCOCC1)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2
CHEMBL3950716 v1ar_human Human No 8.4 IC50 = 4 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
554 8 1 7 5.5 COc1ccc(Cn2c(-c3ccc(Cl)cc3)nn(Cc3nnc(Cc4c(Cl)cccc4Cl)[nH]3)c2=O)cc1
CHEMBL3970631 v1ar_human Human No 8.4 IC50 = 4 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
651 9 3 8 4.7 CC(C)(C)OC(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1C(F)(F)F
CHEMBL4114132 v1ar_human Human No 8.4 IC50 = 4 nM Bind
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
566 9 3 7 3.0 O=C(Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)N[C@@H](CO)Cc1cccc(C(F)(F)F)c1
CHEMBL317243 v1ar_human Human No 8.4 IC50 = 4 nM Funct
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
612 8 2 4 6.6 CN(C)CCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2
CHEMBL318083 v1ar_human Human No 8.4 IC50 = 4 nM Funct
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
582 8 2 4 5.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCCN(C)C)CC3)Cc3ccccc32)cc1
CHEMBL320416 v1ar_human Human No 8.4 IC50 = 4 nM Bind
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V1a receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V1a receptor
539 3 1 3 6.6 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1C(F)(F)F
CHEMBL3963751 v1ar_human Human No 8.4 IC50 = 4.2 nM Bind
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
530 7 1 6 5.4 O=c1n(Cc2nnc(Cc3c(Cl)cccc3Cl)[nH]2)nc(-c2ccc(Cl)cc2)n1CCC(F)(F)F
CHEMBL1837040 v1ar_human Human No 8.3 IC50 = 4.8 nM Funct
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
422 2 0 6 3.6 CC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1
CHEMBL4746818 v1ar_human Human No 7.4 IC50 = 40 nM Funct
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
479 3 0 3 5.0 Cc1ccccc1N1CCN(C(=O)C2CN(C(=O)C3CCCCC3)Cc3cc(Cl)ccc32)CC1
CHEMBL4758799 v1ar_human Human No 7.4 IC50 = 40 nM Funct
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
370 1 1 3 3.5 Cc1ccccc1N1CCN(C(=O)N2CNCc3cc(Cl)ccc32)CC1
CHEMBL4790970 v1ar_human Human No 7.4 IC50 = 40 nM Funct
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
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
CHEMBL242534 v1ar_human Human No 7.4 IC50 = 40 nM Bind
Binding affinity for human cloned vasopressin V1a receptor expressed in CHO cellsBinding affinity for human cloned vasopressin V1a receptor expressed in CHO cells
571 10 1 4 5.9 CC(C)C[C@@H](C(=O)NCc1cccc(Cl)c1)N1C(=O)[C@@H](N2C(=O)OC[C@@H]2c2ccccc2)[C@H]1/C=C/c1ccccc1
CHEMBL49824 v1ar_rat Rat No 7.4 IC50 = 40 nM Bind
Displacement of (Phe-3,4,5 [3H]-) AVP from isolated rat hepatic V1a receptorDisplacement of (Phe-3,4,5 [3H]-) AVP from isolated rat hepatic V1a receptor
460 3 1 4 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1c(F)cccc1Cl
CHEMBL249536 v1ar_human Human No 7.4 IC50 = 40 nM Bind
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cells
532 4 1 4 6.2 COC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3Cl)cc1)c1ccccc1C2
CHEMBL242516 v1ar_human Human No 6.4 IC50 = 400 nM Bind
Binding affinity for human cloned vasopressin V1a receptor expressed in CHO cellsBinding affinity for human cloned vasopressin V1a receptor expressed in CHO cells
482 8 0 5 4.2 O=C(CN1C(=O)[C@@H](N2C(=O)OC[C@@H]2c2ccccc2)[C@H]1/C=C/c1ccccc1)OCc1ccccc1
CHEMBL71712 v1ar_rat Rat No 6.4 IC50 = 400 nM Bind
Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
450 3 1 3 6.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Sc3ccccc32)cc1
CHEMBL2112248 v1ar_rat Rat No 5.4 IC50 = 4000 nM Bind
Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCC=NN2C1=O
CHEMBL118892 v1ar_rat Rat Yes 5.4 IC50 = 4000 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
346 3 1 3 4.1 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccco1
CHEMBL242733 v1ar_human Human No 6.4 IC50 = 405 nM Bind
Binding affinity for human cloned vasopressin V1a receptor expressed in CHO cellsBinding affinity for human cloned vasopressin V1a receptor expressed in CHO cells
578 10 0 7 4.5 CC1(C(C(=O)OCC[Si](C)(C)C)N2C(=O)[C@@H](N3C(=O)OC[C@@H]3c3ccccc3)[C@H]2/C=C/c2ccccc2)OCCO1
CHEMBL1083703 v1ar_human Human No 7.4 IC50 = 41 nM Funct
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
419 3 0 3 6.6 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1csc2ccccc12
CHEMBL244865 v1ar_human Human No 7.4 IC50 = 41 nM Bind
Binding affinity for human cloned vasopressin V1a receptor expressed in CHO cellsBinding affinity for human cloned vasopressin V1a receptor expressed in CHO cells
605 10 1 4 6.2 CC(C)C[C@@H](C(=O)NCc1cccc(C(F)(F)F)c1)N1C(=O)[C@@H](N2C(=O)OC[C@@H]2c2ccccc2)[C@H]1/C=C/c1ccccc1
CHEMBL430676 v1ar_human Human No 7.4 IC50 = 41 nM Bind
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptor
496 5 1 4 6.3 COc1cccc(OC)c1C(=O)Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1
CHEMBL119806 v1ar_rat Rat No 6.4 IC50 = 410 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
398 3 1 2 5.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCCc3ccccc32)cc1
CHEMBL49429 v1ar_rat Rat Yes 6.4 IC50 = 410 nM Bind
Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C
CHEMBL349506 v1ar_human Human No 5.4 IC50 = 4100 nM Bind
In vitro binding affinity to human V1a receptorIn vitro binding affinity to human V1a receptor
496 3 1 5 5.9 Cn1cc2c(n1)-c1sccc1N(C(=O)c1ccc(NC(=O)c3ccc(Cl)cc3Cl)cc1)CC2
CHEMBL280356 v1ar_rat Rat No 5.4 IC50 = 4100 nM Bind
Inhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptorInhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptor
557 7 2 6 2.3 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(NCC(=O)O)C1=O)C2
CHEMBL20205 v1ar_rat Rat No 5.4 IC50 = 4140 nM Bind
Inhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptorInhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptor
482 4 0 4 3.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C=CC1=O)C2
CHEMBL60954 v1ar_rat Rat No 6.4 IC50 = 420 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
435 6 1 4 2.8 CC(=O)NCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL64695 v1ar_rat Rat No 6.4 IC50 = 420 nM Bind
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
406 6 0 3 4.5 CCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1
CHEMBL397188 v1ar_human Human No 7.4 IC50 = 43 nM Bind
Binding affinity for human cloned vasopressin V1a receptor expressed in CHO cellsBinding affinity for human cloned vasopressin V1a receptor expressed in CHO cells
567 9 1 6 3.9 CC1(C(C(=O)NCc2ccccc2)N2C(=O)[C@@H](N3C(=O)OC[C@@H]3c3ccccc3)[C@H]2/C=C/c2ccccc2)OCCO1
CHEMBL297293 v1ar_human Human No 7.4 IC50 = 43 nM Bind
In vitro inhibition of [3H]- AVP binding to V1a receptor from human platelet membraneIn vitro inhibition of [3H]- AVP binding to V1a receptor from human platelet membrane
492 3 1 3 7.1 O=C(Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl
CHEMBL311931 v1ar_human Human No 6.4 IC50 = 430 nM Bind
Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.
469 3 1 3 6.2 Cc1cccc(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)c1C
CHEMBL115434 v1ar_rat Rat Yes 5.4 IC50 = 4300 nM Bind
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liverDisplacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
322 4 1 2 4.0 CCCC(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1
CHEMBL1788221 v1ar_rat Rat No 6.4 IC50 = 433 nM Bind
Evaluated for binding affinity towards vasopressin receptor V1a in ratEvaluated for binding affinity towards vasopressin receptor V1a in rat
554 7 2 4 5.1 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2