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Compound Detail

CHEMBL496127

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N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)Nc1c2c(nc3ccccc13)CCCC2

Basic Information

ChEMBL ID CHEMBL496127
Phase Preclinical
Structure Type MOL
InChI Key JIZMQSOCFUDZSD-NRFANRHFSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

455.6
MW (Da)
3.61
ALogP
4
HBA
4
HBD
112.9
PSA (Ų)
0.34
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H29N5O2
MW 455.56
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -0.68

Activity Summary

Ki 2 meas. best 6.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL1914
Ki 6.76 6.76 173.0 1
Acetylcholinesterase
CHEMBL220
Ki 4.47 4.47 34030.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase Ki = 173.0 nM 6.76 Inhibition of human recombinant BChE 18786825
Acetylcholinesterase Ki = 34030.0 nM 4.47 Inhibition of human recombinant AChE 18786825

Literature References

PubMed DOI Target Context # Activities
18786825 10.1016/j.bmcl.2008.08.076 Acetylcholinesterase 1
18786825 10.1016/j.bmcl.2008.08.076 Cholinesterase 1
18786825 10.1016/j.bmcl.2008.08.076 Cholinesterases; ACHE & BCHE 1

Data from ChEMBL 36 via Core Engine