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Compound Detail

CHEMBL218007

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CC(C)(C)CNc1nc(C#N)ncc1C(=O)NCCc1ccc(OCCn2ccnc2)cc1

Basic Information

ChEMBL ID CHEMBL218007
Phase Preclinical
Structure Type MOL
InChI Key HWNYTOPEHDSGOF-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
2
PK Parameters
6
Publications
0
Known Names

Molecular Properties

447.5
MW (Da)
3.05
ALogP
8
HBA
2
HBD
117.8
PSA (Ų)
0.49
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29N7O2
MW 447.54
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.48

Activity Summary

IC50 3 meas. best 9.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Procathepsin L
CHEMBL3837
IC50 9.28 9.28 0.5 1
Cathepsin S
CHEMBL2954
IC50 9.05 9.05 0.9 1

Pharmacokinetic Data

Parameter Value Units Species
CL 461.67 mL.min-1.kg-1 Rattus norvegicus
T1/2 0.8 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Procathepsin L IC50 = 0.52 nM 9.28 Inhibition of human recombinant cathepsin L 17256925
Cathepsin S IC50 = 0.9 nM 9.05 Inhibition of human recombinant cathepsin S 17256925

Literature References

PubMed DOI Target Context # Activities
17256925 10.1021/jm0613525 Rattus norvegicus 2
17256925 10.1021/jm0613525 Cathepsin K 1
17256925 10.1021/jm0613525 Procathepsin L 1
17256925 10.1021/jm0613525 Cathepsin S 1
17256925 10.1021/jm0613525 Cathepsin (L and K) 1
17256925 10.1021/jm0613525 Cathepsin (S and K) 1

Data from ChEMBL 36 via Core Engine