vasopressin [Ligand Id: 2168] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL373742 (Beta-Hypophamine, Vasostrict, Arginine vasopressin, Leiormone, Vasophysin, Arginine Vasopressin, Vasopressin injection, Pitressin, Vasopressin)
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  • V1A receptor/Vasopressin V1a receptor in Human [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288]
  • V1A receptor/Vasopressin V1a receptor in Rat [ChEMBL: CHEMBL2868] [GtoPdb: 366] [UniProtKB: P30560]
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  • V1B receptor/Vasopressin V1b receptor in Human [ChEMBL: CHEMBL1921] [GtoPdb: 367] [UniProtKB: P47901]
  • V1B receptor/Vasopressin V1b receptor in Rat [ChEMBL: CHEMBL2659] [GtoPdb: 367] [UniProtKB: P48974]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
OT receptor/Oxytocin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2049] [GtoPdb: 369] [UniProtKB: P30559]
ChEMBL Displacement of [3H]OT from oxytocin receptor expressed in COS1 cells B 7.92 pKi 12 nM Ki J. Med. Chem. (2010) 53: 8585-8596 [PMID:21117646]
ChEMBL Displacement of [3H]OT from human mammary gland oxytocin receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method B 8.22 pKi 6 nM Ki Bioorg Med Chem (2018) 26: 3039-3045 [PMID:29602673]
ChEMBL Displacement of [3H]OT from recombinant human OTR expressed in HEK293 cell membranes measured after 1 hr B 8.7 pKi 2 nM Ki J Med Chem (2019) 62: 3297-3310 [PMID:30896946]
ChEMBL Displacement of [3H]AVP from human oxytocin receptor expressed CHO cells after 60 mins B 8.77 pKi 1.7 nM Ki J. Med. Chem. (2011) 54: 2864-2877 [PMID:21428295]
ChEMBL Displacement of [3H]-AVP from human oxytocin receptor expressed in CHO cells after 30 mins B 8.78 pKi 1.65 nM Ki J. Med. Chem. (2012) 55: 8588-8602 [PMID:22984902]
GtoPdb - - 9.3 pKi - - - Life Sci (1995) 57: 2253-61 [PMID:7475979];
EMBO J (1995) 14: 2176-82 [PMID:7774575];
FEBS Lett (1996) 397: 201-6 [PMID:8955347];
J Biol Chem (2001) 276: 26931-41 [PMID:11337500];
Endocrinology (2002) 143: 4655-64 [PMID:12446593];
J Med Chem (2004) 47: 2375-2388 [PMID:15084136];
Br J Pharmacol (2005) 146: 744-751 [PMID:16158071];
Br J Obstet Gynaecol (1999) 106: 1047-53 [PMID:10519430]
ChEMBL Activity at oxytocin receptor expressed in COS1 cells assessed as IP-one generation by HTRF assay B 7.39 pEC50 41 nM EC50 J. Med. Chem. (2010) 53: 8585-8596 [PMID:21117646]
ChEMBL Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay B 7.66 pEC50 22 nM EC50 J. Med. Chem. (2014) 57: 5306-5317 [PMID:24874785]
ChEMBL Agonist activity at human OT receptor expressed in CHO-K1 cells by luciferase reporter gene assay F 7.82 pEC50 15.14 nM EC50 J. Med. Chem. (2011) 54: 4388-4398 [PMID:21688787]
ChEMBL Agonist activity at human OT receptor expressed in CHO-K1 cells by luciferase reporter gene assay F 7.82 pEC50 15 nM EC50 J. Med. Chem. (2011) 54: 4388-4398 [PMID:21688787]
ChEMBL Agonist activity at human oxytocin receptor expressed CHO cells assessed as induction of phospholipase C activity after 15 mins by inositol phosphate accumulation assay F 8.08 pEC50 8.3 nM EC50 J. Med. Chem. (2011) 54: 2864-2877 [PMID:21428295]
ChEMBL Agonist activity at recombinant human OTR 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 B 10 pEC50 0.1 nM EC50 J Med Chem (2019) 62: 3297-3310 [PMID:30896946]
OT receptor/Oxytocin receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3996] [GtoPdb: 369] [UniProtKB: P70536]
ChEMBL Displacement of [3H]AVP from rat OT receptor expressed in CHO cells B 8.93 pKi 1.17 nM Ki J. Med. Chem. (2007) 50: 835-847 [PMID:17300166]
V1A receptor/Vasopressin V1a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288]
ChEMBL Inhibition of human vasopressin V1a receptor expressed in COS7 cells by HTRF-FRET assay using 384-well plate membranes B 8.4 pKi 3.95 nM Ki J. Med. Chem. (2007) 50: 4976-4985 [PMID:17850055]
ChEMBL Displacement of [3H]AVP from human liver vasopressin V1a receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method B 8.7 pKi 2 nM Ki Bioorg Med Chem (2018) 26: 3039-3045 [PMID:29602673]
ChEMBL Inhibition of human vasopressin V1a receptor expressed in COS7 cells by HTRF-FRET assay using 96-well plate membranes B 8.82 pKi 1.53 nM Ki J. Med. Chem. (2007) 50: 4976-4985 [PMID:17850055]
ChEMBL Inhibition of human vasopressin V1a receptor expressed in COS7 cells by HTRF-FRET assay using 96-well plate cells B 8.87 pKi 1.35 nM Ki J. Med. Chem. (2007) 50: 4976-4985 [PMID:17850055]
ChEMBL Inhibition of human vasopressin V1a receptor expressed in COS7 cells by fluorescent binding assay using 384-well plate membranes B 8.89 pKi 1.3 nM Ki J. Med. Chem. (2007) 50: 4976-4985 [PMID:17850055]
ChEMBL Inhibition of human vasopressin V1a receptor expressed in COS7 cells by fluorescent binding assay using 96-well plate membranes B 8.95 pKi 1.13 nM Ki J. Med. Chem. (2007) 50: 4976-4985 [PMID:17850055]
ChEMBL Displacement of [3H]AVP from human vasopressin V1a receptor expressed CHO cells after 60 mins B 8.96 pKi 1.1 nM Ki J. Med. Chem. (2011) 54: 2864-2877 [PMID:21428295]
ChEMBL Displacement of [3H]-AVP from human vasopressin V1a receptor expressed in CHO cells after 30 mins B 9.15 pKi 0.7 nM Ki J. Med. Chem. (2012) 55: 8588-8602 [PMID:22984902]
ChEMBL Inhibition of human vasopressin V1a receptor expressed in COS7 cells by fluorescent binding assay using 96-well plate cells B 9.25 pKi 0.56 nM Ki J. Med. Chem. (2007) 50: 4976-4985 [PMID:17850055]
GtoPdb - - 9.3 pKi - - - Br J Obstet Gynaecol (1999) 106: 1047-53 [PMID:10519430];
J Med Chem (2004) 47: 2375-2388 [PMID:15084136];
Eur J Biochem (2000) 267: 4253-63 [PMID:10866830];
Endocrinology (2002) 143: 4655-64 [PMID:12446593];
Br J Pharmacol (2000) 129: 1700-6 [PMID:10780976];
J Biol Chem (1997) 272: 26536-44 [PMID:9334232];
Biochem Pharmacol (1997) 53: 1711-1717 [PMID:9264324];
Br J Pharmacol (1998) 125: 1463-70 [PMID:9884074];
Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 63-9 [PMID:9459574];
J Biol Chem (1994) 269: 3304-10 [PMID:8106369];
Endocrinology (1997) 138: 4109-22 [PMID:9322919];
J Pharmacol Exp Ther (1998) 287: 860-7 [PMID:9864265]
ChEMBL Inhibition of human vasopressin V1a receptor expressed in CHO cells by polarisation binding assay using 384-well plate membranes B 9.46 pKi 0.35 nM Ki J. Med. Chem. (2007) 50: 4976-4985 [PMID:17850055]
ChEMBL Inhibition of human vasopressin V1a receptor expressed in CHO cells by polarisation binding assay using 96-well plate membranes B 9.59 pKi 0.26 nM Ki J. Med. Chem. (2007) 50: 4976-4985 [PMID:17850055]
ChEMBL Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay F 9.62 pEC50 0.24 nM EC50 J. Med. Chem. (2011) 54: 4388-4398 [PMID:21688787]
ChEMBL Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay B 9.62 pEC50 0.24 nM EC50 J. Med. Chem. (2014) 57: 5306-5317 [PMID:24874785]
ChEMBL Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay F 9.63 pEC50 0.23 nM EC50 J. Med. Chem. (2011) 54: 4388-4398 [PMID:21688787]
V1A receptor/Vasopressin V1a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2868] [GtoPdb: 366] [UniProtKB: P30560]
ChEMBL Negative log of Kd. B 9.19 pKd 0.65 nM Kd J. Med. Chem. (1992) 35: 151-157 [PMID:1732523]
ChEMBL Binding potency against V1 receptor in rat liver cells B 9.19 pKd 0.64 nM Kd J. Med. Chem. (1992) 35: 151-157 [PMID:1732523]
GtoPdb - - 8.4 pKi - - - EMBO J (1995) 14: 2176-82 [PMID:7774575]
ChEMBL Displacement of [3H]AVP from vasopressin V1a receptor in rat liver membrane B 8.81 pKi 1.54 nM Ki J. Med. Chem. (2007) 50: 835-847 [PMID:17300166]
ChEMBL Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay F 10.15 pEC50 0.07 nM EC50 J. Med. Chem. (2011) 54: 4388-4398 [PMID:21688787]
ChEMBL Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay F 10.2 pEC50 0.06 nM EC50 J. Med. Chem. (2011) 54: 4388-4398 [PMID:21688787]
V1B receptor/Vasopressin V1b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1921] [GtoPdb: 367] [UniProtKB: P47901]
ChEMBL Displacement of [3H]AVP from human vasopressin V1b receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method B 8.7 pKi 2 nM Ki Bioorg Med Chem (2018) 26: 3039-3045 [PMID:29602673]
ChEMBL Displacement of [3H]AVP from human vasopressin V1b receptor expressed CHO cells after 60 mins B 9.17 pKi 0.68 nM Ki J. Med. Chem. (2011) 54: 2864-2877 [PMID:21428295]
ChEMBL Displacement of [3H]-AVP from human vasopressin V1b receptor expressed in CHO cells after 30 mins B 9.31 pKi 0.49 nM Ki J. Med. Chem. (2012) 55: 8588-8602 [PMID:22984902]
GtoPdb - - 9.5 pKi - - - Br J Obstet Gynaecol (1999) 106: 1047-53 [PMID:10519430];
J Med Chem (2004) 47: 2375-2388 [PMID:15084136];
Endocrinology (2002) 143: 4655-64 [PMID:12446593];
Br J Pharmacol (2005) 146: 744-751 [PMID:16158071];
Br J Pharmacol (2000) 129: 1700-6 [PMID:10780976];
Biochem Pharmacol (1997) 53: 1711-1717 [PMID:9264324];
Br J Pharmacol (1998) 125: 1463-70 [PMID:9884074];
Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 63-9 [PMID:9459574];
Endocrinology (1997) 138: 4109-22 [PMID:9322919];
J Pharmacol Exp Ther (1998) 287: 860-7 [PMID:9864265]
ChEMBL Agonist activity at recombinant human vasopressin V1b receptor expressed in Flp-In-293 cells by luciferase reporter gene assay F 8.37 pEC50 4.3 nM EC50 J. Med. Chem. (2011) 54: 4388-4398 [PMID:21688787]
ChEMBL Agonist activity at human vasopressin V1b expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay B 8.37 pEC50 4.3 nM EC50 J. Med. Chem. (2014) 57: 5306-5317 [PMID:24874785]
ChEMBL Agonist activity at recombinant human vasopressin V1b receptor expressed in Flp-In-293 cells by luciferase reporter gene assay F 8.37 pEC50 4.27 nM EC50 J. Med. Chem. (2011) 54: 4388-4398 [PMID:21688787]
ChEMBL Agonist activity at human vasopressin V1b receptor expressed CHO cells assessed as induction of phospholipase C activity after 15 mins by inositol phosphate accumulation assay F 8.7 pEC50 2 nM EC50 J. Med. Chem. (2011) 54: 2864-2877 [PMID:21428295]
V1B receptor/Vasopressin V1b receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2659] [GtoPdb: 367] [UniProtKB: P48974]
ChEMBL Displacement of [3H]AVP from rat vasopressin V1b receptor expressed in At-T20 cells B 9.54 pKi 0.29 nM Ki J. Med. Chem. (2007) 50: 835-847 [PMID:17300166]
GtoPdb - - 9.9 pKi - - - Biochem Pharmacol (1997) 53: 1711-1717 [PMID:9264324]
V2 receptor/Vasopressin V2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1790] [GtoPdb: 368] [UniProtKB: P30518]
ChEMBL Displacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method B 7.49 pKi 32 nM Ki Bioorg Med Chem (2018) 26: 3039-3045 [PMID:29602673]
ChEMBL Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins B 8.83 pKi 1.48 nM Ki J. Med. Chem. (2012) 55: 8588-8602 [PMID:22984902]
ChEMBL Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assay B 8.87 pKi 1.36 nM Ki J. Med. Chem. (2012) 55: 8588-8602 [PMID:22984902]
ChEMBL Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins B 8.92 pKi 1.2 nM Ki J. Med. Chem. (2011) 54: 2864-2877 [PMID:21428295]
GtoPdb - - 9.1 pKi - - - Br J Obstet Gynaecol (1999) 106: 1047-53 [PMID:10519430];
J Med Chem (2004) 47: 2375-2388 [PMID:15084136];
EMBO J (1995) 14: 2176-82 [PMID:7774575];
Endocrinology (2002) 143: 4655-64 [PMID:12446593];
Br J Pharmacol (2000) 129: 1700-6 [PMID:10780976];
Biochem Pharmacol (1997) 53: 1711-1717 [PMID:9264324];
Kidney Int (2000) 58: 1613-22 [PMID:11012895];
Br J Pharmacol (1998) 125: 1463-70 [PMID:9884074];
Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 63-9 [PMID:9459574];
Endocrinology (1997) 138: 4109-22 [PMID:9322919];
J Pharmacol Exp Ther (1998) 287: 860-7 [PMID:9864265]
ChEMBL Binding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assay B 6.62 pIC50 242 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 989-995 [PMID:23312470]
ChEMBL Binding to human V2 receptor expressed in LV2 cells by cAMP production B 10.28 pEC50 0.05 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 954-959 [PMID:16297621]
ChEMBL Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay F 10.3 pEC50 0.05 nM EC50 J. Med. Chem. (2011) 54: 4388-4398 [PMID:21688787]
ChEMBL Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay F 10.3 pEC50 0.05 nM EC50 J. Med. Chem. (2011) 54: 4388-4398 [PMID:21688787]
ChEMBL Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay B 10.3 pEC50 0.05 nM EC50 J. Med. Chem. (2014) 57: 5306-5317 [PMID:24874785]
Vasopressin V2 receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3944] [UniProtKB: P32307]
ChEMBL Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells B 8.48 pIC50 3.3 nM IC50 Bioorg. Med. Chem. Lett. (1997) 7: 719-724
Vasopressin V2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2344] [UniProtKB: P48044]
ChEMBL Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane B 8.82 pKd 1.5 nM Kd J. Med. Chem. (1994) 37: 255-259 [PMID:7507528]
V2 receptor/Vasopressin V2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3766] [GtoPdb: 368] [UniProtKB: Q00788]
ChEMBL Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor B 8.82 pKd 1.5 nM Kd Bioorg. Med. Chem. Lett. (1999) 9: 667-672 [PMID:10201826]
ChEMBL Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes B 9.35 pKi 0.45 nM Ki J. Med. Chem. (2007) 50: 835-847 [PMID:17300166]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]