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, Inyectable de vasopresina, Leiormone, Pitressin, Solute injectable de vasopressine, 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 | - | - | - |
Endocrinology (2002) 143: 4655-64 [PMID:12446593]; J Med Chem (2004) 47: 2375-2388 [PMID:15084136]; Br J Obstet Gynaecol (1999) 106: 1047-53 [PMID:10519430]; EMBO J (1995) 14: 2176-82 [PMID:7774575]; J Biol Chem (2001) 276: 26931-41 [PMID:11337500]; Br J Pharmacol (2005) 146: 744-751 [PMID:16158071]; Life Sci (1995) 57: 2253-61 [PMID:7475979]; FEBS Lett (1996) 397: 201-6 [PMID:8955347] |
| 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 | Activation of human 3X-HA N-tagged AVP1a expressed in CHO-K1 cells incubated for 10 mins by cell Western assay | B | 7.49 | pEC50 | 32 | nM | EC50 | ACS Med Chem Lett (2023) 14: 163-170 [PMID:36793431] |
| ChEMBL | Agonist activity at human V1a receptor transfected in HEK293 cells incubated for 1 hr by IP-one HTRF assay | F | 9.19 | pEC50 | 0.64 | nM | EC50 | J Med Chem (2023) 66: 14853-14865 [PMID:37857356] |
| 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 | Activation of human 3X-HA N-tagged AVP1b expressed in CHO-K1 cells incubated for 10 mins by cell Western assay | B | 7.96 | pEC50 | 11 | nM | EC50 | ACS Med Chem Lett (2023) 14: 163-170 [PMID:36793431] |
| 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 V1b receptor transfected in HEK293 cells incubated for 1 hr by IP-one HTRF assay | F | 8.48 | pEC50 | 3.33 | nM | EC50 | J Med Chem (2023) 66: 14853-14865 [PMID:37857356] |
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
