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Compound Detail

CHEMBL2164684

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N#CC1(NC(=O)[C@@H]2CCCC[C@H]2C(=O)N2CCc3[nH]c4cc(F)ccc4c3C2)CC1

Basic Information

ChEMBL ID CHEMBL2164684
Phase Preclinical
Structure Type MOL
InChI Key MIOKYZZTPMKVEG-IAGOWNOFSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
7
Publications
0
Known Names

Molecular Properties

408.5
MW (Da)
3.17
ALogP
3
HBA
2
HBD
89.0
PSA (Ų)
0.82
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25FN4O2
MW 408.48
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -1.30

Activity Summary

IC50 1 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
IC50 8.4 8.4 4.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 89.0 mL.min-1.g-1 Rattus norvegicus
CL 36.0 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 = 4.0 nM 8.4 Inhibition of human recombinant CatK assessed as suppression of enzyme-mediated ... 22742641

Literature References

PubMed DOI Target Context # Activities
22742641 10.1021/jm3007257 Liver microsomes 2
22742641 10.1021/jm3007257 No relevant target 2
- 10.6019/CHEMBL3301361 No relevant target 2
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