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Compound Detail

CHEMBL3099497

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Nc1cccc2c(NCCCCCCCCNc3c4c(nc5ccccc35)CCCC4)c3c(nc12)CCCC3

Basic Information

ChEMBL ID CHEMBL3099497
Phase Preclinical
Structure Type MOL
InChI Key GVQOVWDFVYXHFJ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

521.8
MW (Da)
7.99
ALogP
5
HBA
3
HBD
75.9
PSA (Ų)
0.14
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H43N5
MW 521.75
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -0.44

Activity Summary

Ki 2 meas. best 9.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
Ki 9.64 9.64 0.2 1
Cholinesterase
CHEMBL1914
Ki 8.08 8.08 8.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase Ki = 0.23 nM 9.64 Inhibition of human acetylcholine esterase 24900626
Cholinesterase Ki = 8.26 nM 8.08 Inhibition of human butyrylcholine 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