carbetocin [Ligand Id: 11169] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3301668 (Carbetocin, Carbetocina, Carbetocine, 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 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]
