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Compound Detail

CHEMBL4859103

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CC1=CC2Cc3nc4cc(Cl)ccc4c(NCCCCCCCCCNC(=O)c4cc(O)cc(O)c4)c3C(C1)C2

Basic Information

ChEMBL ID CHEMBL4859103
Phase Preclinical
Structure Type MOL
InChI Key LODADOWHBHYNFI-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

562.1
MW (Da)
7.87
ALogP
5
HBA
4
HBD
94.5
PSA (Ų)
0.13
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H40ClN3O3
MW 562.15
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -0.11

Activity Summary

IC50 3 meas. best 8.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 8.59 8.59 2.6 1
Cholinesterase
CHEMBL1914
IC50 7.37 7.37 43.0 1
Beta-secretase 1
CHEMBL4822
IC50 5.57 5.57 2710.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34418785 10.1016/j.ejmech.2021.113779 Mus musculus 13
34418785 10.1016/j.ejmech.2021.113779 ADMET 6
34418785 10.1016/j.ejmech.2021.113779 Unchecked 5
34418785 10.1016/j.ejmech.2021.113779 Cholinesterase 4
34418785 10.1016/j.ejmech.2021.113779 Acetylcholinesterase 3
34418785 10.1016/j.ejmech.2021.113779 No relevant target 2
34418785 10.1016/j.ejmech.2021.113779 Beta-secretase 1 1
34418785 10.1016/j.ejmech.2021.113779 Amyloid-beta precursor protein 1
34418785 10.1016/j.ejmech.2021.113779 Microtubule-associated protein tau 1
34418785 10.1016/j.ejmech.2021.113779 HT-22 1

Data from ChEMBL 36 via Core Engine