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Compound Detail

CHEMBL2163581

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CS(=O)(=O)c1ccc2[nH]c3c(c2c1)CN(C(=O)[C@@H]1CCCC[C@H]1C(=O)NC1(C#N)CC1)CC3

Basic Information

ChEMBL ID CHEMBL2163581
Phase Preclinical
Structure Type MOL
InChI Key LOXUZEQLPYVKQR-IAGOWNOFSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
8
Publications
0
Known Names

Molecular Properties

468.6
MW (Da)
2.43
ALogP
5
HBA
2
HBD
123.1
PSA (Ų)
0.71
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H28N4O4S
MW 468.58
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.38

Activity Summary

IC50 1 meas. best 7.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
IC50 7.11 7.11 78.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 14.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin K IC50 = 78.0 nM 7.11 Inhibition of human recombinant CatK assessed as suppression of enzyme-mediated ... 22742641

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3301361 No relevant target 2
22742641 10.1021/jm3007257 Hepatocyte 1
22742641 10.1021/jm3007257 Liver microsomes 1
22742641 10.1021/jm3007257 No relevant target 1
22742641 10.1021/jm3007257 Cathepsin B 1
22742641 10.1021/jm3007257 Cathepsin S 1
22742641 10.1021/jm3007257 Procathepsin L 1
22742641 10.1021/jm3007257 Cathepsin K 1

Data from ChEMBL 36 via Core Engine