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 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]
