vibegron [Ligand Id: 10100] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2107826 (Gemtesa, KRP-114V, Mk4618, Vibegron) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
| ChEMBL | Displacement of [125]I-cyanopindolol from recombinant human beta1 adrenergic receptor after 1 hr by scintillation counting method | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2016) 59: 609-623 [PMID:26709102] |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
| ChEMBL | Displacement of [125]I-cyanopindolol from human recombinant beta2 adrenergic receptor after 1 hr by scintillation counting method | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2016) 59: 609-623 [PMID:26709102] |
| β3-adrenoceptor in Monkey [GtoPdb: 30] | ||||||||
| GtoPdb | - | - | 9.24 | pEC50 | 0.57 | nM | EC50 | J Med Chem (2016) 59: 609-23 [PMID:26709102] |
| Beta-3 adrenergic receptor in Rhesus macaque (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3124732] [UniProtKB: Q28524] | ||||||||
| ChEMBL | Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum | F | 8.15 | pEC50 | 7.1 | nM | EC50 | J Med Chem (2016) 59: 609-623 [PMID:26709102] |
| ChEMBL | Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | F | 9.24 | pEC50 | 0.57 | nM | EC50 | J Med Chem (2016) 59: 609-623 [PMID:26709102] |
| β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945] | ||||||||
| ChEMBL | Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum | F | 8.8 | pEC50 | 1.6 | nM | EC50 | J Med Chem (2016) 59: 609-623 [PMID:26709102] |
| ChEMBL | Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | F | 8.96 | pEC50 | 1.1 | nM | EC50 | J Med Chem (2016) 59: 609-623 [PMID:26709102] |
| GtoPdb | - | - | 9 | pEC50 | - | - | - |
J Med Chem (2016) 59: 609-23 [PMID:26709102]; J Pharmacol Exp Ther (2017) 360: 346-355 [PMID:27965369]; Curr Ther Res Clin Exp (2022) 96: 100674 [PMID:35693456] |
| Beta-3 adrenergic receptor in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4400] [UniProtKB: O02662] | ||||||||
| ChEMBL | Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | F | 7.96 | pEC50 | 11 | nM | EC50 | J Med Chem (2016) 59: 609-623 [PMID:26709102] |
| β3-adrenoceptor/Beta-3 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4031] [GtoPdb: 30] [UniProtKB: P26255] | ||||||||
| ChEMBL | Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum | F | 6.91 | pEC50 | 122 | nM | EC50 | J Med Chem (2016) 59: 609-623 [PMID:26709102] |
| ChEMBL | Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | F | 7.07 | pEC50 | 86 | nM | EC50 | J Med Chem (2016) 59: 609-623 [PMID:26709102] |
| GtoPdb | - | - | 7.07 | pEC50 | 86 | nM | EC50 | J Med Chem (2016) 59: 609-23 [PMID:26709102] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Binding affinity to human ERG channel | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2016) 59: 609-623 [PMID:26709102] |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | Inhibition of human SERT expressed in HEK293 cells preincubated for 30 mins followed by fluorescent substrate addition measured after 30 mins by plate reader analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 609-623 [PMID:26709102] |
| Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524] | ||||||||
| ChEMBL | Inhibition of human Nav1.2 channel expressed in Xenopus oocytes by two-intracellular microelectrode voltage clamp method | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2016) 59: 609-623 [PMID:26709102] |
| Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936] | ||||||||
| ChEMBL | Displacement of [3H]-diltiazem from human Cav1.2 channel | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2016) 59: 609-623 [PMID:26709102] |
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]
