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Compound Detail

CHEMBL401986

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Cc1c(C(=O)N[C@@H](Cc2ccccc2)C(=O)C(=O)NCCc2ccccc2)[nH]c2ccccc2c1=O

Basic Information

ChEMBL ID CHEMBL401986
Phase Preclinical
Structure Type MOL
InChI Key GTWQVINVJBGZNG-DEOSSOPVSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

481.6
MW (Da)
3.11
ALogP
4
HBA
3
HBD
108.1
PSA (Ų)
0.32
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H27N3O4
MW 481.55
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -0.36

Activity Summary

IC50 1 meas. best 5.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Calpain-1 catalytic subunit
CHEMBL3891
IC50 5.43 5.43 3710.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Calpain-1 catalytic subunit IC50 = 3710.0 nM 5.43 Inhibition of human mu-calpain 18024028

Literature References

PubMed DOI Target Context # Activities
36827952 10.1016/j.ejmech.2023.115211 Leishmania donovani 2
18024028 10.1016/j.bmcl.2007.10.097 Calpain-1 catalytic subunit 1
36827952 10.1016/j.ejmech.2023.115211 THP-1 1
36827952 10.1016/j.ejmech.2023.115211 HEK-293T 1

Data from ChEMBL 36 via Core Engine