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Compound Detail

CHEMBL436302

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CCOC(=O)C1=C(C)Nc2nc3c(c(N)c2C1c1ccccc1OC)CCCC3

Basic Information

ChEMBL ID CHEMBL436302
Phase Preclinical
Structure Type MOL
InChI Key RYUHYOLRLQUVHQ-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
18
Publications
0
Known Names

Molecular Properties

393.5
MW (Da)
3.95
ALogP
6
HBA
2
HBD
86.5
PSA (Ų)
0.77
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H27N3O3
MW 393.49
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.66

Activity Summary

IC50 4 meas. best 6.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL4078
IC50 6.8 6.8 160.0 2
Acetylcholinesterase
CHEMBL220
IC50 6.63 6.63 234.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17181144 10.1021/jm061047j SH-SY5Y 4
17181144 10.1021/jm061047j Unchecked 2
19374444 10.1021/jm801292b SH-SY5Y 2
19374444 10.1021/jm801292b Acetylcholinesterase 2
17181144 10.1021/jm061047j Acetylcholinesterase 2
19374444 10.1021/jm801292b Cholinesterase 1
- 10.6019/CHEMBL4513135 HEK293 1
- 10.6019/CHEMBL4513135 Staphylococcus aureus 1
- 10.6019/CHEMBL4513135 Acinetobacter baumannii 1
- 10.6019/CHEMBL4513135 Pseudomonas aeruginosa 1
- 10.6019/CHEMBL4513135 Klebsiella pneumoniae 1
- 10.6019/CHEMBL4513135 Escherichia coli 1
- 10.6019/CHEMBL4513135 Cryptococcus neoformans 1
- 10.6019/CHEMBL4513135 Candida albicans 1
19374444 10.1021/jm801292b Voltage-gated L-type calcium channel 1
19374444 10.1021/jm801292b ADMET 1
19374444 10.1021/jm801292b Cholinesterases; ACHE & BCHE 1
17181144 10.1021/jm061047j Cholinesterase 1

Data from ChEMBL 36 via Core Engine