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Compound Detail

CHEMBL3099496

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O=[N+]([O-])c1cccc2c(NCCCCCCCCNc3c4c(nc5ccccc35)CCCC4)c3c(nc12)CCCC3

Basic Information

ChEMBL ID CHEMBL3099496
Phase Preclinical
Structure Type MOL
InChI Key DMTOWVUOHDLGGK-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

551.7
MW (Da)
8.31
ALogP
6
HBA
2
HBD
93.0
PSA (Ų)
0.10
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H41N5O2
MW 551.74
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -0.69

Activity Summary

Ki 2 meas. best 10.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL1914
Ki 10.22 10.22 0.1 1
Acetylcholinesterase
CHEMBL220
Ki 9.11 9.11 0.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase Ki = 0.06 nM 10.22 Inhibition of human butyrylcholine esterase 24900626
Acetylcholinesterase Ki = 0.78 nM 9.11 Inhibition of human acetylcholine esterase 24900626

Literature References

PubMed DOI Target Context # Activities
24900626 10.1021/ml4002908 Acetylcholinesterase 2
24900626 10.1021/ml4002908 Amyloid-beta precursor protein 1
24900626 10.1021/ml4002908 Unchecked 1
24900626 10.1021/ml4002908 Cholinesterase 1

Data from ChEMBL 36 via Core Engine