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Compound Detail

CHEMBL211737

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CC(C)CC(C(=O)NCC#N)c1cccc(-c2ccc(-c3csc(N4CCNCC4)n3)cc2)c1

Basic Information

ChEMBL ID CHEMBL211737
Phase Preclinical
Structure Type MOL
InChI Key BJXUTJHNAOJFQL-UHFFFAOYSA-N
5
Targets
5
Activities
2
Assay Types
2
PK Parameters
9
Publications
0
Known Names

Molecular Properties

473.6
MW (Da)
4.66
ALogP
6
HBA
2
HBD
81.0
PSA (Ų)
0.47
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H31N5OS
MW 473.65
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.29

Activity Summary

Ki 4 meas. best 8.46
IC50 1 meas. best 7.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
Ki 8.46 8.46 3.5 1
Osteoclast
CHEMBL612548
IC50 7.92 7.92 12.0 1
Procathepsin L
CHEMBL3837
Ki 5.6 5.6 2500.0 1
Cathepsin S
CHEMBL2954
Ki 5.02 5.02 9500.0 1
Cathepsin B
CHEMBL4072
Ki 4.92 4.92 12000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 114.0 mL.min-1.kg-1 Rattus norvegicus
MRT 1.767 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16750630 10.1016/j.bmcl.2006.05.061 Rattus norvegicus 3
16750630 10.1016/j.bmcl.2006.05.061 Cathepsin (S and K) 1
16750630 10.1016/j.bmcl.2006.05.061 Cathepsin (B and K) 1
16750630 10.1016/j.bmcl.2006.05.061 Cathepsin (L and K) 1
16750630 10.1016/j.bmcl.2006.05.061 Osteoclast 1
16750630 10.1016/j.bmcl.2006.05.061 Cathepsin S 1
16750630 10.1016/j.bmcl.2006.05.061 Cathepsin B 1
16750630 10.1016/j.bmcl.2006.05.061 Procathepsin L 1
16750630 10.1016/j.bmcl.2006.05.061 Cathepsin K 1

Data from ChEMBL 36 via Core Engine