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Compound Detail

CHEMBL508778

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

Basic Information

ChEMBL ID CHEMBL508778
Phase Preclinical
Structure Type MOL
InChI Key OUAQDAJKPZIRBK-MHZLTWQESA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

555.7
MW (Da)
5.18
ALogP
5
HBA
4
HBD
125.2
PSA (Ų)
0.24
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H37N5O4
MW 555.68
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -0.84

Activity Summary

Ki 2 meas. best 6.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL1914
Ki 6.35 6.35 443.0 1
Acetylcholinesterase
CHEMBL220
Ki 5.1 5.1 7970.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase Ki = 443.0 nM 6.35 Inhibition of human recombinant BChE 18786825
Acetylcholinesterase Ki = 7970.0 nM 5.1 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

Data from ChEMBL 36 via Core Engine