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Compound Detail

CHEMBL4128887

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CC(C)C[C@H](N[C@@H](c1ccc(F)cc1)C(F)(F)F)C(=O)NC1(C#N)CC1

Basic Information

ChEMBL ID CHEMBL4128887
Phase Preclinical
Structure Type MOL
InChI Key AEMUDLMOFLXUQI-GJZGRUSLSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

371.4
MW (Da)
3.61
ALogP
3
HBA
2
HBD
64.9
PSA (Ų)
0.72
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 C18H21F4N3O
MW 371.38
Aromatic Rings 1
Heavy Atoms 26
NP-Likeness -1.01

Activity Summary

IC50 2 meas. best 7.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Procathepsin L
CHEMBL3837
IC50 7.08 7.08 84.0 1
Cathepsin L
CHEMBL4295862
IC50 6.8 6.8 160.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.3667 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29650289 10.1016/j.bmcl.2018.03.020 ADMET 7
29650289 10.1016/j.bmcl.2018.03.020 Cathepsin L 1
29650289 10.1016/j.bmcl.2018.03.020 Procathepsin L 1
29650289 10.1016/j.bmcl.2018.03.020 Unchecked 1
29650289 10.1016/j.bmcl.2018.03.020 No relevant target 1

Data from ChEMBL 36 via Core Engine