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Compound Detail

CHEMBL4212454

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CN(C#N)N(C)C(=O)[C@H](Cc1ccccc1)NC(=O)c1cc(C(C)(C)C)nn1C

Basic Information

ChEMBL ID CHEMBL4212454
Phase Preclinical
Structure Type MOL
InChI Key GWGYOEFAMBIJPC-INIZCTEOSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

396.5
MW (Da)
1.84
ALogP
6
HBA
1
HBD
94.3
PSA (Ų)
0.46
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H28N6O2
MW 396.50
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -1.20

Activity Summary

Ki 4 meas. best 9.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Procathepsin L
CHEMBL3837
Ki 9.9 9.9 0.1 1
Unchecked
CHEMBL612545
Ki 9.7 9.7 0.2 1
Cruzipain
CHEMBL3563
Ki 8.8 8.8 1.6 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29054358 10.1016/j.bmcl.2017.10.002 Cruzipain 4
33038787 10.1016/j.bmc.2020.115743 Unchecked 3
33038787 10.1016/j.bmc.2020.115743 Procathepsin L 3
33038787 10.1016/j.bmc.2020.115743 Cruzipain 3

Data from ChEMBL 36 via Core Engine