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Compound Detail

CHEMBL201178

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CSc1ccc(-c2ccccc2[C@@H]2CCCC[C@H]2C(=O)NCC#N)cc1

Basic Information

ChEMBL ID CHEMBL201178
Phase Preclinical
Structure Type MOL
InChI Key UKQULZSZDDFLST-LEWJYISDSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

364.5
MW (Da)
4.99
ALogP
3
HBA
1
HBD
52.9
PSA (Ų)
0.60
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 C22H24N2OS
MW 364.51
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.75

Activity Summary

IC50 1 meas. best 8.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
IC50 8.59 8.59 2.6 1

Pharmacokinetic Data

Parameter Value Units Species
CL 35.0 mL.min-1.kg-1 Rattus norvegicus
T1/2 0.7333 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin K IC50 = 2.6 nM 8.59 Inhibitory activity against humanized rabbit Cathepsin K 16451072

Literature References

PubMed DOI Target Context # Activities
16451072 10.1021/jm051059p Rattus norvegicus 2
16451072 10.1021/jm051059p Cathepsin K 1
16451072 10.1021/jm051059p Cathepsin (L and K) 1
16451072 10.1021/jm051059p Cathepsin (B and K) 1
16451072 10.1021/jm051059p Cathepsin (S and K) 1

Data from ChEMBL 36 via Core Engine