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Compound Detail

CHEMBL3234040

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CC1=CC2Cc3nc4cc(Cl)ccc4c(NCc4ccc(CNC(=O)c5cc(O)c6c(c5)C(=O)c5cccc(O)c5C6=O)cc4)c3C(C1)C2.Cl

Basic Information

ChEMBL ID CHEMBL3234040
Phase Preclinical
Structure Type MOL
InChI Key RIVZUMYSVIHQNG-UHFFFAOYSA-N
Parent Compound CHEMBL3304178
Active Moiety CHEMBL3304178
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

670.2
MW (Da)
7.61
ALogP
7
HBA
4
HBD
128.6
PSA (Ų)
0.13
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C40H33Cl2N3O5
MW 706.63
Aromatic Rings 5
Heavy Atoms 49
NP-Likeness 0.04

Activity Summary

IC50 3 meas. best 7.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 7.74 7.74 18.2 1
Cholinesterase
CHEMBL1914
IC50 6.29 6.29 510.0 1
Beta-secretase 1
CHEMBL4822
IC50 5.7 5.7 2020.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24568372 10.1021/jm401824w Acetylcholinesterase 2
24568372 10.1021/jm401824w Amyloid-beta precursor protein 2
24568372 10.1021/jm401824w Cholinesterase 1
24568372 10.1021/jm401824w Beta-secretase 1 1
24568372 10.1021/jm401824w No relevant target 1
24568372 10.1021/jm401824w Cholinesterases; ACHE & BCHE 1
24568372 10.1021/jm401824w Microtubule-associated protein tau 1

Data from ChEMBL 36 via Core Engine