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ChEMBL ligand: CHEMBL363910 (VNA-932, WAY-VNA-932) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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OT receptor/Oxytocin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2049] [GtoPdb: 369] [UniProtKB: P30559] | ||||||||
ChEMBL | Displacement of [3H]AVP from human oxytocin receptor expressed in CHO cells | B | 6.7 | pKi | 199 | nM | Ki | J Med Chem (2010) 53: 1546-1562 [PMID:20104850] |
ChEMBL | Displacement of [3H]-AVP from human OXR receptor expressed in CHO cell membranes by radioligand binding assay | B | 6.7 | pKi | 199 | nM | Ki | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
ChEMBL | Binding affinity to OTR receptor (unknown origin) | B | 6.9 | pKi | 125 | nM | Ki | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
ChEMBL | Displacement of [3H]oxytocin from human oxytocin receptor expressed in CHO cells | B | 6.45 | pIC50 | 353 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5796-5800 [PMID:17855087] |
ChEMBL | Activity at human oxytocin receptor expressed in CHO cells by NFAT-luciferase gene reporter assay | B | 6.9 | pEC50 | 125 | nM | EC50 | J Med Chem (2010) 53: 1546-1562 [PMID:20104850] |
OT receptor/Oxytocin receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3996] [GtoPdb: 369] [UniProtKB: P70536] | ||||||||
ChEMBL | Antagonist activity at OXR receptor in rat uterus | F | 7.26 | pIC50 | 55 | nM | IC50 | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
V1A receptor/Vasopressin V1a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288] | ||||||||
ChEMBL | Binding affinity to V1A receptor (unknown origin) | B | 6.33 | pKi | 465 | nM | Ki | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
ChEMBL | Displacement of [3H]AVP from human vasopressin V1a receptor expressed in CHO cells | B | 6.46 | pKi | 344 | nM | Ki | J Med Chem (2010) 53: 1546-1562 [PMID:20104850] |
ChEMBL | Displacement of [3H]-AVP from human V1A receptor expressed in CHO cell membranes by radioligand binding assay | B | 6.46 | pKi | 344 | nM | Ki | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
ChEMBL | Antagonist activity at V1A receptor (unknown origin) by cAMP accumulation assay | F | 5.78 | pIC50 | 1660 | nM | IC50 | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
ChEMBL | Displacement of [3H]AVP from human V1a receptor expressed in CHO cells | B | 6.11 | pIC50 | 778 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 954-959 [PMID:16297621] |
ChEMBL | Displacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cells | B | 6.11 | pIC50 | 778 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5796-5800 [PMID:17855087] |
ChEMBL | Activity at human vasopressin V1a receptor expressed in CHO cells by NFAT-luciferase gene reporter assay | B | 6.33 | pEC50 | 465 | nM | EC50 | J Med Chem (2010) 53: 1546-1562 [PMID:20104850] |
V1B receptor/Vasopressin V1b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1921] [GtoPdb: 367] [UniProtKB: P47901] | ||||||||
ChEMBL | Binding affinity to V1B receptor (unknown origin) | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
V2 receptor/Vasopressin V2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1790] [GtoPdb: 368] [UniProtKB: P30518] | ||||||||
ChEMBL | Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells | B | 7.3 | pKi | 50 | nM | Ki | J Med Chem (2010) 53: 1546-1562 [PMID:20104850] |
ChEMBL | Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay | B | 7.3 | pKi | 50 | nM | Ki | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
ChEMBL | Binding affinity to V2 receptor (unknown origin) | B | 7.4 | pKi | 39.9 | nM | Ki | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
ChEMBL | Displacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cells | B | 7.1 | pIC50 | 80.3 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5796-5800 [PMID:17855087] |
ChEMBL | Displacement of [3H]AVP from human V2 receptor transfected in LV2 cells | B | 7.1 | pIC50 | 80 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 954-959 [PMID:16297621] |
GtoPdb | - | - | 7.1 | pIC50 | 80 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 954-9 [PMID:16297621] |
ChEMBL | Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay | B | 7.4 | pEC50 | 39.9 | nM | EC50 | J Med Chem (2010) 53: 1546-1562 [PMID:20104850] |
ChEMBL | Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay | F | 9 | pEC50 | <1 | nM | EC50 | J Med Chem (2008) 51: 8124-8134 [PMID:19053774] |
ChEMBL | Binding to human V2 receptor expressed in LV2 cells by cAMP production | F | 9.13 | pEC50 | 0.74 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 954-959 [PMID:16297621] |
ChEMBL | Agonist activity at V2 receptor (unknown origin) by cAMP accumulation assay | F | 9.15 | pEC50 | 0.7 | nM | EC50 | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
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]