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Compound Detail

CHEMBL1240874

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COc1nc(N)c2ncn(CCCNC(=O)C(=O)C(Cc3ccccc3)NC(=O)[C@H](CC(C)C)NC(=O)OCc3ccccc3)c2n1

Basic Information

ChEMBL ID CHEMBL1240874
Phase Preclinical
Structure Type MOL
InChI Key LMZPTXHQVRKQEC-BBMPLOMVSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

644.7
MW (Da)
2.56
ALogP
11
HBA
4
HBD
192.4
PSA (Ų)
0.10
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 C33H40N8O6
MW 644.73
Aromatic Rings 4
Heavy Atoms 47
NP-Likeness -0.50

Activity Summary

Ki 3 meas. best 7.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Calpain-1 catalytic subunit
CHEMBL4062
Ki 7.39 7.39 41.0 1
Calpain-2 catalytic subunit
CHEMBL4143
Ki 6.68 6.68 209.0 1
Cathepsin B
CHEMBL4072
Ki 5.63 5.63 2340.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20690647 10.1021/jm901221v Calpain-1 catalytic subunit 2
20690647 10.1021/jm901221v Calpain-2 catalytic subunit 1
20690647 10.1021/jm901221v Cathepsin B 1
20690647 10.1021/jm901221v Unchecked 1

Data from ChEMBL 36 via Core Engine