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Compound Detail

CHEMBL4450266

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CC1CCN(C2CCN(S(=O)(=O)c3ccc(Cl)cc3)CC2)CC1

Basic Information

ChEMBL ID CHEMBL4450266
Phase Preclinical
Structure Type MOL
InChI Key KQARQZVXVMKIER-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
12
PK Parameters
3
Publications
0
Known Names

Molecular Properties

356.9
MW (Da)
3.23
ALogP
3
HBA
0
HBD
40.6
PSA (Ų)
0.83
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H25ClN2O2S
MW 356.92
Aromatic Rings 1
Heavy Atoms 23
NP-Likeness -1.72

Activity Summary

IC50 1 meas. best 8.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DLD-1
CHEMBL614285
IC50 8.66 8.66 2.2 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 359.68 ng.hr.mL-1 Mus musculus
AUClast 262874.0 ng.min/g Mus musculus
CL 2.9 mL.min-1.g-1 Mus musculus
CL 10.6 ml/min Mus musculus
Cmax 535.13 nM Mus musculus
Cmax 1414.0 ng/g Mus musculus
T1/2 0.6833 hr Mus musculus
T1/2 1.35 hr Mus musculus
T1/2 231.02 hr Mus musculus
Tmax 0.5 hr Mus musculus
Tmax 0.1667 hr Mus musculus
Vd 5.87 L.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DLD-1 IC50 = 2.2 nM 8.66 Antiproliferative activity against human DLD1 cells after 72 hrs by Celltiter-Gl... 31070915

Literature References

PubMed DOI Target Context # Activities
31070915 10.1021/acs.jmedchem.9b00532 ADMET 13
31070915 10.1021/acs.jmedchem.9b00532 DLD-1 1
31070915 10.1021/acs.jmedchem.9b00532 HCT-116 1

Data from ChEMBL 36 via Core Engine