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Compound Detail

CHEMBL210712

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CCC[C@H](NC(=O)CCc1ccccc1)C(=O)c1nnc(-c2ccco2)o1

Basic Information

ChEMBL ID CHEMBL210712
Phase Preclinical
Structure Type MOL
InChI Key MJWAQGWWWAVZBT-HNNXBMFYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

367.4
MW (Da)
3.43
ALogP
6
HBA
1
HBD
98.2
PSA (Ų)
0.58
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 C20H21N3O4
MW 367.41
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.03

Activity Summary

Ki 4 meas. best 5.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin S
CHEMBL2954
Ki 5.58 5.58 2600.0 1
Cathepsin K
CHEMBL268
Ki 5.02 5.02 9600.0 1
Cathepsin B
CHEMBL4072
Ki 4.6 4.6 25000.0 1
Procathepsin L
CHEMBL3837
Ki 4.0 4.0 100000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin S Ki = 2600.0 nM 5.58 Inhibition of human cathepsin S 16546382
Cathepsin K Ki = 9600.0 nM 5.02 Inhibition of human cathepsin K 16546382
Cathepsin B Ki = 25000.0 nM 4.6 Inhibition of human cathepsin B 16546382
Procathepsin L Ki = 100000.0 nM 4.0 Inhibition of human cathepsin L 16546382

Literature References

PubMed DOI Target Context # Activities
16546382 10.1016/j.bmcl.2006.03.001 Cathepsin K 1
16546382 10.1016/j.bmcl.2006.03.001 Cathepsin B 1
16546382 10.1016/j.bmcl.2006.03.001 Procathepsin L 1
16546382 10.1016/j.bmcl.2006.03.001 Cathepsin S 1

Data from ChEMBL 36 via Core Engine