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Compound Detail

CHEMBL490236

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OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3Br)(CC1)CC2.[Br-]

Basic Information

ChEMBL ID CHEMBL490236
Phase Preclinical
Structure Type MOL
InChI Key OYRRUMWUKNIZRJ-UHFFFAOYSA-M
Parent Compound CHEMBL1187091
Active Moiety CHEMBL1187091
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

507.5
MW (Da)
5.90
ALogP
2
HBA
1
HBD
29.5
PSA (Ų)
0.30
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H33Br2NO2
MW 587.40
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.18

Activity Summary

IC50 1 meas. best 4.66
Kd 1 meas. best 8.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M3
CHEMBL245
Kd 8.5 8.5 3.2 1
Muscarinic acetylcholine receptor M3
CHEMBL245
IC50 4.66 4.66 22000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19317446 10.1021/jm801601v Muscarinic acetylcholine receptor M3 2

Data from ChEMBL 36 via Core Engine