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Compound Detail

CHEMBL372979

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CC(C)C[C@H](NC(c1ccc(Br)cc1)C(F)(F)F)C(=O)NCC#N

Basic Information

ChEMBL ID CHEMBL372979
Phase Preclinical
Structure Type MOL
InChI Key VPRPGHWVFIVNRD-LSLKUGRBSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

406.2
MW (Da)
3.70
ALogP
3
HBA
2
HBD
64.9
PSA (Ų)
0.68
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H19BrF3N3O
MW 406.25
Aromatic Rings 1
Heavy Atoms 24
NP-Likeness -1.01

Activity Summary

IC50 5 meas. best 9.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
IC50 9.05 8.97 0.9 2
Procathepsin L
CHEMBL3837
IC50 7.47 7.47 34.0 1
Cathepsin S
CHEMBL2954
IC50 6.92 6.92 121.0 1
Cathepsin B
CHEMBL4072
IC50 5.47 5.47 3353.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16154747 10.1016/j.bmcl.2005.07.071 Cathepsin K 3
16154747 10.1016/j.bmcl.2005.07.071 Cathepsin B 1
16154747 10.1016/j.bmcl.2005.07.071 Procathepsin L 1
16154747 10.1016/j.bmcl.2005.07.071 Cathepsin S 1

Data from ChEMBL 36 via Core Engine