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Compound Detail

CHEMBL201016

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C[N+](C)(CC#CCN1OCCC1=O)CCCCCC[N+](C)(C)CCCN1C(=O)c2ccccc2C1=O.[Br-].[Br-]

Basic Information

ChEMBL ID CHEMBL201016
Phase Preclinical
Structure Type MOL
InChI Key NSYYTTOLDWKQNE-UHFFFAOYSA-L
Parent Compound CHEMBL1181949
Active Moiety CHEMBL1181949
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

498.7
MW (Da)
2.55
ALogP
4
HBA
0
HBD
66.9
PSA (Ų)
0.18
QED
0
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H42Br2N4O4
MW 658.48
Aromatic Rings 1
Heavy Atoms 36
NP-Likeness -0.25

Activity Summary

EC50 1 meas. best 7.08
Kd 1 meas. best 4.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M2
CHEMBL4781
EC50 7.08 7.08 83.2 1
Muscarinic acetylcholine receptor M3
CHEMBL5498
Kd 4.35 4.35 44668.4 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

Data from ChEMBL 36 via Core Engine