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Compound Detail

CHEMBL3414841

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C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2c(F)cccc2c1=O.[Br-]

Basic Information

ChEMBL ID CHEMBL3414841
Phase Preclinical
Structure Type MOL
InChI Key JBXNSUQULFZCSQ-UHFFFAOYSA-N
Parent Compound CHEMBL3559128
Active Moiety CHEMBL3559128
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

561.7
MW (Da)
4.31
ALogP
6
HBA
1
HBD
81.9
PSA (Ų)
0.20
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H38BrFN4O4
MW 641.58
Aromatic Rings 3
Heavy Atoms 41
NP-Likeness -0.69

Activity Summary

EC50 1 meas. best 6.75
Kd 1 meas. best 6.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M1
CHEMBL216
EC50 6.75 6.75 177.8 1
Muscarinic acetylcholine receptor M1
CHEMBL216
Kd 6.31 6.31 489.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25478907 10.1021/jm500860w Muscarinic acetylcholine receptor M1 11

Data from ChEMBL 36 via Core Engine