Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL3833319

REVEFENACIN
💊 Approved Drug
Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
💊 Approved Drug
CN(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)C(=O)c1ccc(CN2CCC(C(N)=O)CC2)cc1

Basic Information

ChEMBL ID CHEMBL3833319
Name REVEFENACIN
Phase Approved
Structure Type MOL
InChI Key FYDWDCIFZSGNBU-UHFFFAOYSA-N
Therapeutic ✓ Yes

Known Names

GSK-1160724 GSK1160724 Revefenacin Revefenacina Revefenacine TD-4208 Yupelri
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
20
Publications
7
Known Names
4
Indications
1
Mechanisms

Molecular Properties

597.8
MW (Da)
4.84
ALogP
6
HBA
2
HBD
108.2
PSA (Ų)
0.35
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 2018
Availability Prescription
Chirality Achiral

Routes of Administration

Topical

Flags

Natural Product
USAN Stem -fenacin
USAN Year 2016

Extended Properties

Molecular Formula C35H43N5O4
MW 597.76
Aromatic Rings 3
Heavy Atoms 44
NP-Likeness -1.30

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Muscarinic acetylcholine receptor M3 antagonist ANTAGONIST Muscarinic acetylcholine receptor M3

Indications

Lung Diseases, Obstructive Pulmonary Disease, Chronic Obstructive Kidney Diseases Liver Diseases

ATC Classification

R03BB08
revefenacin
Level 1: RESPIRATORY SYSTEM
Level 2: DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES

Activity Summary

IC50 1 meas. best 7.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M2
CHEMBL211
IC50 7.33 7.33 46.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Muscarinic acetylcholine receptor M2 IC50 = 46.88 nM 7.33 GPCR PRESTO-Tango dose-response in antagonist mode with target: CHRM2 -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5058564 Fibroblast 8
- 10.6019/CHEMBL5058564 HEK-293T 8
- 10.6019/CHEMBL5209801 Glucagon-like peptide 1 receptor 2
- 10.6019/CHEMBL5209801 G-protein coupled receptor 35 2
- 10.6019/CHEMBL5209801 Free fatty acid receptor 4 2
- 10.6019/CHEMBL5209801 Apelin receptor 2
- 10.6019/CHEMBL5209801 Adhesion G-protein coupled receptor F1 2
- 10.6019/CHEMBL5209801 C5a anaphylatoxin chemotactic receptor 1 2
- 10.6019/CHEMBL5209801 Type-1 angiotensin II receptor 2
- 10.6019/CHEMBL5209801 Alpha-2A adrenergic receptor 2
- 10.6019/CHEMBL5209801 Sphingosine 1-phosphate receptor 1 2
- 10.6019/CHEMBL5209801 Beta-2 adrenergic receptor 2
- 10.6019/CHEMBL5209801 Glucose-dependent insulinotropic receptor 2
- 10.6019/CHEMBL5209801 N-formyl peptide receptor 2 2
- 10.6019/CHEMBL5209801 CX3C chemokine receptor 1 2
- 10.6019/CHEMBL5058564 U2OS 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL5060014 Fibroblast growth factor receptor 3 1
- 10.6019/CHEMBL5060014 Glycogen synthase kinase-3 beta 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1

Data from ChEMBL 36 via Core Engine