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Compound Detail

CHEMBL383612

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CSc1ccc(-c2ccccc2C2CCC(Cl)(Cl)CC2C(=O)NCC#N)cc1

Basic Information

ChEMBL ID CHEMBL383612
Phase Preclinical
Structure Type MOL
InChI Key GLZDKRQTDOWMEO-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
3
PK Parameters
5
Publications
0
Known Names

Molecular Properties

433.4
MW (Da)
5.77
ALogP
3
HBA
1
HBD
52.9
PSA (Ų)
0.37
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22Cl2N2OS
MW 433.40
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -0.52

Activity Summary

IC50 2 meas. best 9.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
IC50 9.24 9.24 0.6 1
Cathepsin K
CHEMBL3349
IC50 9.23 9.23 0.6 1

Pharmacokinetic Data

Parameter Value Units Species
CL 51.0 mL.min-1.kg-1 Rattus norvegicus
F 75.0 % Rattus norvegicus
T1/2 3.1 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin K IC50 = 0.58 nM 9.24 Inhibitory activity against humanized rabbit Cathepsin K 16451072
Cathepsin K IC50 = 0.59 nM 9.23 Inhibitory activity against rabbit Cathepsin K 16451072

Literature References

PubMed DOI Target Context # Activities
16451072 10.1021/jm051059p Rattus norvegicus 3
16451072 10.1021/jm051059p Cathepsin K 2
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