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Compound Detail

CHEMBL233611

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CCN(CC)Cc1ccc(C(=O)N(CCc2ccccc2OC)[C@@H]2CCNC2)cc1

Basic Information

ChEMBL ID CHEMBL233611
Phase Preclinical
Structure Type MOL
InChI Key XKPJTOHUPQWSOJ-HSZRJFAPSA-N
7
Targets
9
Activities
2
Assay Types
2
PK Parameters
14
Publications
0
Known Names

Molecular Properties

409.6
MW (Da)
3.58
ALogP
4
HBA
1
HBD
44.8
PSA (Ų)
0.65
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H35N3O2
MW 409.57
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -1.10

Activity Summary

EC50 6 meas. best 6.52
IC50 3 meas. best 6.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Membrane-bound transcription factor site-1 protease
CHEMBL5916
IC50 6.77 6.77 170.0 1
Hepatocyte
CHEMBL3140324
EC50 6.52 6.11 300.0 2
Liver
CHEMBL613580
EC50 6.52 6.11 300.0 2
HepG2
CHEMBL395
EC50 6.22 6.22 600.0 1
Liver
CHEMBL613642
EC50 6.22 6.22 600.0 1
Urokinase-type plasminogen activator
CHEMBL3286
IC50 4.3 4.3 50000.0 1
Coagulation factor X
CHEMBL244
IC50 4.0 4.0 100000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 75.0 mL.min-1.kg-1 Rattus norvegicus
F 5.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35752380 10.1016/j.bmcl.2022.128866 Unchecked 13
17583500 10.1016/j.bmcl.2007.06.031 Mus musculus 9
17583500 10.1016/j.bmcl.2007.06.031 HepG2 5
17583500 10.1016/j.bmcl.2007.06.031 Liver 4
17583500 10.1016/j.bmcl.2007.06.031 Rattus norvegicus 2
17583500 10.1016/j.bmcl.2007.06.031 Hepatocyte 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
17583500 10.1016/j.bmcl.2007.06.031 Membrane-bound transcription factor site-1 protease 1
17583500 10.1016/j.bmcl.2007.06.031 Urokinase-type plasminogen activator 1
17583500 10.1016/j.bmcl.2007.06.031 Coagulation factor X 1
17583500 10.1016/j.bmcl.2007.06.031 Low-density lipoprotein receptor 1
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1

Data from ChEMBL 36 via Core Engine