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Compound Detail

CHEMBL3261928

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CN1Cc2ccc(-c3ccc(C[C@@H](C#N)NC(=O)C4(N)CCOCC4)cc3)cc2C1=O

Basic Information

ChEMBL ID CHEMBL3261928
Phase Preclinical
Structure Type MOL
InChI Key ALYPEORYGVOPDI-FQEVSTJZSA-N
2
Targets
3
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

418.5
MW (Da)
2.00
ALogP
5
HBA
2
HBD
108.5
PSA (Ų)
0.77
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 C24H26N4O3
MW 418.50
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -0.18

Activity Summary

IC50 3 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 1
CHEMBL2252
IC50 8.3 7.8 5.0 2
Cathepsin K
CHEMBL268
IC50 5.1 5.1 7943.3 1

Pharmacokinetic Data

Parameter Value Units Species
CL 3.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24592859 10.1021/jm401705g Dipeptidyl peptidase 1 2
24592859 10.1021/jm401705g No relevant target 2
24592859 10.1021/jm401705g Cathepsin K 2
24592859 10.1021/jm401705g ADMET 1
24592859 10.1021/jm401705g Hepatocyte 1
24592859 10.1021/jm401705g Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine