vasopressin [Ligand Id: 2168] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL373742 (Arginine vasopressin, Arginine Vasopressin, Argipressin or lypressin, Beta-Hypophamine, Leiormone, Pitressin, Vasophysin, Vasopressin, Vasopressin injection, Vasopressin, unspecified, Vasostrict) |
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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 | F | 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 | F | 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
