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ChEMBL ligand: CHEMBL2107826 (KRP-114V, Vibegron, MK-4618) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | pIC50 | 0.57 | nM | IC50 | 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 | B | 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 | B | 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 | B | 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 | B | 8.96 | pEC50 | 1.1 | nM | EC50 | J. Med. Chem. (2016) 59: 609-623 [PMID:26709102] |
GtoPdb | - | - | 8.96 | pEC50 | 1.1 | nM | EC50 | J. Med. Chem. (2016) 59: 609-23 [PMID:26709102] |
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 | B | 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 | B | 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 | B | 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 27:
Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]