carbetocin [Ligand Id: 11169] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3301668 (Carbetocin, Duratocin, Duratocin long acting, FE 992097, FE-992097, LV-101, Pabal) |
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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 recombinant human OTR expressed in HEK293 cell membranes measured after 1 hr | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (2019) 62: 3297-3310 [PMID:30896946] |
| ChEMBL | Agonist activity at human OTR receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay | F | 7.39 | pEC50 | 41 | nM | EC50 | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| GtoPdb | Agonist activity at hOT receptor receptor expressed in HEK293FT cells by beta-arrestin recruitment assay. | - | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| ChEMBL | Agonist activity at human OTR receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay | F | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| ChEMBL | Agonist activity at recombinant human Gi/Go-coupled OTR expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins in presence of 10% FBS by pathhunter assay | B | 8.52 | pEC50 | 2.99 | nM | EC50 | J Med Chem (2020) 63: 382-390 [PMID:31850759] |
| ChEMBL | Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay | B | 9.15 | pEC50 | 0.7 | nM | EC50 | J Med Chem (2014) 57: 5306-5317 [PMID:24874785] |
| 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 | 11 | pEC50 | 0.01 | nM | EC50 | J Med Chem (2019) 62: 3297-3310 [PMID:30896946] |
| OT receptor/Oxytocin receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3243907] [GtoPdb: 369] [UniProtKB: P97926] | ||||||||
| ChEMBL | Agonist activity at mouse OTR receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay | F | 7.21 | pEC50 | 62 | nM | EC50 | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| GtoPdb | Agonist activity at MmOT receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay. | - | 7.21 | pEC50 | 62 | nM | EC50 | 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 | Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2014) 57: 5306-5317 [PMID:24874785] |
| ChEMBL | Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay | B | 7.39 | pEC50 | 41 | nM | EC50 | J Med Chem (2014) 57: 5306-5317 [PMID:24874785] |
| V1B receptor/Vasopressin V1b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1921] [GtoPdb: 367] [UniProtKB: P47901] | ||||||||
| ChEMBL | Agonist activity at human V1b receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay | F | 4.57 | pEC50 | 27000 | nM | EC50 | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| ChEMBL | Agonist activity at human vasopressin V1b expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2014) 57: 5306-5317 [PMID:24874785] |
| V2 receptor/Vasopressin V2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1790] [GtoPdb: 368] [UniProtKB: P30518] | ||||||||
| ChEMBL | Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay | F | 5.17 | pEC50 | 6700 | nM | EC50 | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| ChEMBL | Agonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay | F | 5.96 | pEC50 | 1100 | nM | EC50 | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| ChEMBL | Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay | B | 6.77 | pEC50 | 170 | nM | EC50 | J Med Chem (2014) 57: 5306-5317 [PMID:24874785] |
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]
