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Compound Detail

CHEMBL3960432

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Cc1cc(-c2ccc(C[C@@H](C#N)NC(=O)[C@@H]3CNCCCO3)cc2)cc2c1oc(=O)n2C

Basic Information

ChEMBL ID CHEMBL3960432
Phase Preclinical
Structure Type MOL
InChI Key WCWJGAFMGPMBQG-FPOVZHCZSA-N
1
Targets
9
Activities
1
Assay Types
8
PK Parameters
7
Publications
0
Known Names

Molecular Properties

434.5
MW (Da)
2.04
ALogP
7
HBA
2
HBD
109.3
PSA (Ų)
0.64
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 C24H26N4O4
MW 434.50
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.55

Activity Summary

IC50 9 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 1
CHEMBL2252
IC50 8.1 8.0033 7.9 9

Pharmacokinetic Data

Parameter Value Units Species
CL 14.0 mL.min-1.g-1 Homo sapiens
CL - - Canis lupus familiaris
CL 1.0 mL.min-1.kg-1 Rattus norvegicus
F - % Canis lupus familiaris
F 24.0 % Rattus norvegicus
T1/2 50.0 hr -
t1/2 - - Canis lupus familiaris
T1/2 8.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27690432 10.1021/acs.jmedchem.6b01127 ADMET 12
27690432 10.1021/acs.jmedchem.6b01127 Molecular identity unknown 3
27690432 10.1021/acs.jmedchem.6b01127 NON-PROTEIN TARGET 3
27690432 10.1021/acs.jmedchem.6b01127 Dipeptidyl peptidase 1 2
27690432 10.1021/acs.jmedchem.6b01127 No relevant target 2
27690432 10.1021/acs.jmedchem.6b01127 Unchecked 1
27690432 10.1021/acs.jmedchem.6b01127 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine