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Compound Detail

CHEMBL4857068

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COc1ccc(-c2ccc(C(=O)N(CC(=O)NC3(C#N)CC3)Cc3ccccc3)cc2)cc1

Basic Information

ChEMBL ID CHEMBL4857068
Phase Preclinical
Structure Type MOL
InChI Key TYMYINLXOFGBOV-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

439.5
MW (Da)
4.18
ALogP
4
HBA
1
HBD
82.4
PSA (Ų)
0.57
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H25N3O3
MW 439.52
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.25

Activity Summary

Ki 3 meas. best 5.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin S
CHEMBL2954
Ki 5.4 5.4 3981.1 1
Cathepsin K
CHEMBL268
Ki 5.0 5.0 10000.0 1
Cruzipain
CHEMBL3563
Ki 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33991733 10.1016/j.bmc.2021.116211 Cruzipain 1
33991733 10.1016/j.bmc.2021.116211 Cathepsin K 1
33991733 10.1016/j.bmc.2021.116211 Cathepsin S 1
33991733 10.1016/j.bmc.2021.116211 Procathepsin L 1
33991733 10.1016/j.bmc.2021.116211 Cathepsin B 1

Data from ChEMBL 36 via Core Engine