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Compound Detail

CHEMBL382846

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C[N+](C)(CC#CCOc1ccon1)CCCCCC[N+](C)(C)CCCN1C(=O)c2ccccc2C1=O.[Br-].[Br-]

Basic Information

ChEMBL ID CHEMBL382846
Phase Preclinical
Structure Type MOL
InChI Key BXBQGCJIUWCZHF-UHFFFAOYSA-L
Parent Compound CHEMBL1185000
Active Moiety CHEMBL1185000
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

496.6
MW (Da)
3.46
ALogP
5
HBA
0
HBD
72.6
PSA (Ų)
0.17
QED
0
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H40Br2N4O4
MW 656.46
Aromatic Rings 2
Heavy Atoms 36
NP-Likeness -0.47

Activity Summary

EC50 1 meas. best 7.3
IC50 1 meas. best 4.41

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M2
CHEMBL4781
EC50 7.3 7.3 50.1 1
Cholinesterase
CHEMBL5763
IC50 4.41 4.41 38904.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16392821 10.1021/jm050769s Muscarinic acetylcholine receptor M2 4
16392821 10.1021/jm050769s Muscarinic acetylcholine receptor M1 2
16392821 10.1021/jm050769s Muscarinic acetylcholine receptor M3 2
30108847 10.1039/C7MD00149E Acetylcholinesterase 2
30108847 10.1039/C7MD00149E Cholinesterase 2
30108847 10.1039/C7MD00149E HepG2 1
30108847 10.1039/C7MD00149E No relevant target 1

Data from ChEMBL 36 via Core Engine