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Compound Detail

CHEMBL223170

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N#Cc1ccc2[nH]cc(CCC(=O)NCCCCCCNc3c4c(nc5cc(Cl)ccc35)CCCC4)c2c1

Basic Information

ChEMBL ID CHEMBL223170
Phase Preclinical
Structure Type MOL
InChI Key PBSOJOMZHQNAPL-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

528.1
MW (Da)
6.84
ALogP
4
HBA
3
HBD
93.6
PSA (Ų)
0.19
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 C31H34ClN5O
MW 528.10
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.07

Activity Summary

IC50 3 meas. best 9.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 9.15 9.15 0.7 1
Acetylcholinesterase
CHEMBL4768
IC50 9.15 9.15 0.7 1
Cholinesterase
CHEMBL1914
IC50 7.93 7.93 11.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 0.7 nM 9.15 Inhibition of AchE in bovine erythrocytes 16279781
Acetylcholinesterase IC50 = 0.7 nM 9.15 Inhibition of AChE 20053484
Cholinesterase IC50 = 11.7 nM 7.93 Inhibition of human serum BChE 16279781

Literature References

PubMed DOI Target Context # Activities
16279781 10.1021/jm0503289 Acetylcholinesterase 1
16279781 10.1021/jm0503289 Cholinesterase 1
16279781 10.1021/jm0503289 Unchecked 1
20053484 10.1016/j.ejmech.2009.12.038 Acetylcholinesterase 1

Data from ChEMBL 36 via Core Engine