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Compound Detail

CHEMBL1790994

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CC[C@@H](C)[C@H](/N=C(\S)Nc1cccc2ccccc12)C(=O)N[C@@H](C=O)Cc1c[nH]c2ccccc12

Basic Information

ChEMBL ID CHEMBL1790994
Phase Preclinical
Structure Type MOL
InChI Key ZDJKOPMEVPPKBM-OFUUFJSKSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

486.6
MW (Da)
5.36
ALogP
3
HBA
4
HBD
86.3
PSA (Ų)
0.11
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H30N4O2S
MW 486.64
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.23

Activity Summary

IC50 2 meas. best 8.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Procathepsin L
CHEMBL3837
IC50 8.35 8.35 4.5 1
Cathepsin B
CHEMBL4072
IC50 6.51 6.51 310.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Procathepsin L IC50 = 4.5 nM 8.35 Inhibition of human cathepsin L. 9784105
Cathepsin B IC50 = 310.0 nM 6.51 Inhibition of human cathepsin B 9784105

Literature References

PubMed DOI Target Context # Activities
9784105 10.1021/jm9803065 Procathepsin L 1
9784105 10.1021/jm9803065 Cathepsin B 1
9784105 10.1021/jm9803065 Unchecked 1

Data from ChEMBL 36 via Core Engine