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Compound Detail

CHEMBL4861956

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COc1ccc2[nH]c(C(=O)Nc3ccc4nc5n(c(=O)c4c3)CCC5)cc2c1

Basic Information

ChEMBL ID CHEMBL4861956
Phase Preclinical
Structure Type MOL
InChI Key BCHSBAPBQXDRKS-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

374.4
MW (Da)
3.08
ALogP
5
HBA
2
HBD
89.0
PSA (Ų)
0.58
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H18N4O3
MW 374.40
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -1.49

Activity Summary

IC50 4 meas. best 6.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 6.92 6.92 120.0 1
Acetylcholinesterase
CHEMBL4078
IC50 6.92 6.92 120.0 1
Cholinesterase
CHEMBL5763
IC50 6.82 6.82 150.0 1
Amyloid-beta precursor protein
CHEMBL2487
IC50 5.92 5.92 1210.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34153471 10.1016/j.bmcl.2021.128212 Acetylcholinesterase 4
34153471 10.1016/j.bmcl.2021.128212 Cholinesterase 1
34153471 10.1016/j.bmcl.2021.128212 Amyloid-beta precursor protein 1
34153471 10.1016/j.bmcl.2021.128212 PC-12 1
34153471 10.1016/j.bmcl.2021.128212 BV-2 1
38052155 10.1016/j.ejmech.2023.116013 Acetylcholinesterase 1

Data from ChEMBL 36 via Core Engine