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Compound Detail

CHEMBL200151

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N#CCNC(=O)C1(NC(=O)OCc2ccccc2)CCCCC1

Basic Information

ChEMBL ID CHEMBL200151
Phase Preclinical
Structure Type MOL
InChI Key KYSYABZOHYNMCH-UHFFFAOYSA-N
6
Targets
8
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

315.4
MW (Da)
2.26
ALogP
4
HBA
2
HBD
91.2
PSA (Ų)
0.82
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H21N3O3
MW 315.37
Aromatic Rings 1
Heavy Atoms 23
NP-Likeness -1.00

Activity Summary

Ki 8 meas. best 7.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL3349
Ki 7.08 7.08 84.0 1
Falcipain 2
CHEMBL5800
Ki 5.92 5.92 1200.0 1
Unchecked
CHEMBL612545
Ki 5.92 5.92 1200.0 1
Procathepsin L
CHEMBL3837
Ki 4.58 4.3933 26500.0 3
Cathepsin S
CHEMBL2954
Ki 4.51 4.51 31000.0 1
Cathepsin B
CHEMBL4072
Ki 4.19 4.19 64000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C1MD00115A Unchecked 3
- 10.1039/C1MD00115A Cathepsin B 2
- 10.1039/C1MD00115A Procathepsin L 2
36996716 10.1016/j.ejmech.2023.115299 Unchecked 2
16302794 10.1021/jm058198r Cathepsin K 1
16302794 10.1021/jm058198r Cathepsin B 1
16302794 10.1021/jm058198r Procathepsin L 1
16302794 10.1021/jm058198r Cathepsin S 1
26985300 10.1021/acsmedchemlett.5b00474 Cathepsin B 1
27890381 10.1016/j.bmcl.2016.11.036 Unchecked 1
27890381 10.1016/j.bmcl.2016.11.036 Procathepsin L 1
36996716 10.1016/j.ejmech.2023.115299 Falcipain 2 1
36996716 10.1016/j.ejmech.2023.115299 Procathepsin L 1

Data from ChEMBL 36 via Core Engine