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Compound Detail

CHEMBL2107826

VIBEGRON
💊 Approved Drug
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💊 Approved Drug
O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)[C@@H]1CCc2nccc(=O)n21

Basic Information

ChEMBL ID CHEMBL2107826
Name VIBEGRON
Phase Approved
Structure Type MOL
InChI Key DJXRIQMCROIRCZ-XOEOCAAJSA-N
Therapeutic ✓ Yes

Known Names

Gemtesa KRP-114V Mk4618 Obgemsa Vibegron
4
Targets
7
Activities
1
Assay Types
24
PK Parameters
20
Publications
5
Known Names
6
Indications
1
Mechanisms

Molecular Properties

444.5
MW (Da)
2.77
ALogP
6
HBA
3
HBD
96.2
PSA (Ų)
0.54
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 2018
Availability Prescription
Chirality Single Enantiomer

Routes of Administration

Oral
USAN Stem -begron
USAN Year 2012

Extended Properties

Molecular Formula C26H28N4O3
MW 444.54
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.25

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Beta-3 adrenergic receptor agonist AGONIST Beta-3 adrenergic receptor

Indications

Polyuria Urinary Bladder, Overactive Urinary Incontinence Urinary Incontinence, Urge Irritable Bowel Syndrome Hypertension

ATC Classification

G04BD15
vibegron
Level 1: GENITO URINARY SYSTEM AND SEX HORMONES
Level 2: UROLOGICALS

Activity Summary

EC50 7 meas. best 9.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-3 adrenergic receptor
CHEMBL3124732
EC50 9.24 8.695 0.6 2
Beta-3 adrenergic receptor
CHEMBL246
EC50 8.96 8.88 1.1 2
Beta-3 adrenergic receptor
CHEMBL4400
EC50 7.96 7.96 11.0 1
Beta-3 adrenergic receptor
CHEMBL4031
EC50 7.07 6.99 86.0 2

Pharmacokinetic Data

Parameter Value Units Species
CL 14.0 mL.min-1.kg-1 Rattus norvegicus
CL 15.0 mL.min-1.kg-1 Canis lupus familiaris
CL 16.0 mL.min-1.kg-1 Macaca mulatta
CL 67.0 mL.min-1.kg-1 Rattus norvegicus
CL 37.0 mL.min-1.kg-1 Canis lupus familiaris
CL 33.0 mL.min-1.kg-1 Macaca mulatta
CL 10.0 mL.min-1.kg-1 Homo sapiens
CL 20.0 mL.min-1.kg-1 Rattus norvegicus
CL 13.0 mL.min-1.kg-1 Canis lupus familiaris
CL 18.0 mL.min-1.kg-1 Macaca mulatta
CL 20.0 mL.min-1.kg-1 Macaca fascicularis
CL 34.0 mL.min-1.kg-1 Macaca fascicularis
F 20.0 % Rattus norvegicus
F 44.0 % Canis lupus familiaris
F 23.0 % Macaca mulatta
F 46.0 % Macaca fascicularis
Fu 0.21 - Rattus norvegicus
Fu 0.41 - Canis lupus familiaris
Fu 0.49 - Macaca mulatta
Fu 0.58 - Macaca fascicularis
T1/2 7.0 hr Rattus norvegicus
T1/2 13.0 hr Canis lupus familiaris
T1/2 14.0 hr Macaca mulatta
T1/2 7.0 hr Macaca fascicularis

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26709102 10.1021/acs.jmedchem.5b01372 Rattus norvegicus 16
26709102 10.1021/acs.jmedchem.5b01372 ADMET 15
26709102 10.1021/acs.jmedchem.5b01372 Beta-3 adrenergic receptor 13
26709102 10.1021/acs.jmedchem.5b01372 Cynomolgus monkey 8
26709102 10.1021/acs.jmedchem.5b01372 Rhesus monkey 6
26709102 10.1021/acs.jmedchem.5b01372 Canis familiaris 6
26709102 10.1021/acs.jmedchem.5b01372 Plasma 4
26709102 10.1021/acs.jmedchem.5b01372 NON-PROTEIN TARGET 4
26709102 10.1021/acs.jmedchem.5b01372 Cytochrome P450 3A4 3
26709102 10.1021/acs.jmedchem.5b01372 Liver microsome 3
26709102 10.1021/acs.jmedchem.5b01372 No relevant target 3
26709102 10.1021/acs.jmedchem.5b01372 Sodium-dependent serotonin transporter 1
26709102 10.1021/acs.jmedchem.5b01372 Cytochrome P450 2C19 1
26709102 10.1021/acs.jmedchem.5b01372 HepG2 1
26709102 10.1021/acs.jmedchem.5b01372 Sodium channel protein type 5 subunit alpha 1
26709102 10.1021/acs.jmedchem.5b01372 Voltage-dependent L-type calcium channel subunit alpha-1C 1
26709102 10.1021/acs.jmedchem.5b01372 Voltage-gated inwardly rectifying potassium channel KCNH2 1
26709102 10.1021/acs.jmedchem.5b01372 Cytochrome P450 2D6 1
26709102 10.1021/acs.jmedchem.5b01372 Cytochrome P450 2C9 1
26709102 10.1021/acs.jmedchem.5b01372 Beta-2 adrenergic receptor 1

Data from ChEMBL 36 via Core Engine