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Compound Detail

CHEMBL575674

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CCC1=CC2Cc3nc4cc(Cl)ccc4c(NCCn4cc(CCCCCCN5CCc6cc(OC)c(OC)cc6C5c5cccc([N+](=O)[O-])c5)nn4)c3C(C1)C2

Basic Information

ChEMBL ID CHEMBL575674
Phase Preclinical
Structure Type MOL
InChI Key DRYDFCTXPZWATR-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

790.4
MW (Da)
9.65
ALogP
10
HBA
1
HBD
120.5
PSA (Ų)
0.05
QED
2
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C45H52ClN7O4
MW 790.41
Aromatic Rings 5
Heavy Atoms 57
NP-Likeness -0.71

Activity Summary

IC50 1 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 8.22 8.22 6.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 5.96 nM 8.22 Inhibition of human recombinant AChE in erythrocytes by Ellman's assay 19473849

Literature References

PubMed DOI Target Context # Activities
19473849 10.1016/j.bmc.2009.05.005 Unchecked 1
19473849 10.1016/j.bmc.2009.05.005 Acetylcholinesterase 1
19473849 10.1016/j.bmc.2009.05.005 Cholinesterase 1

Data from ChEMBL 36 via Core Engine