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Compound Detail

CHEMBL4561814

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O=C1CCC(N2Cc3c(SCc4ccc(C(=O)N5CCCCC5)cc4)cccc3C2=O)C(=O)N1

Basic Information

ChEMBL ID CHEMBL4561814
Phase Preclinical
Structure Type MOL
InChI Key YREZRIBYHQVZCY-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
8
PK Parameters
2
Publications
0
Known Names

Molecular Properties

477.6
MW (Da)
3.37
ALogP
5
HBA
1
HBD
86.8
PSA (Ų)
0.53
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H27N3O4S
MW 477.59
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.75

Activity Summary

IC50 1 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 9.3 9.3 0.5 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 34.1 ng.hr.mL-1 Mus musculus
AUC 424.0 ng.hr.mL-1 Mus musculus
CL 197.0 mL.min-1.kg-1 Mus musculus
Cmax 34.97 nM Mus musculus
F 2.9 % Mus musculus
MRT 0.45 hr Mus musculus
T1/2 0.7 hr Mus musculus
Tmax 0.5 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 0.5 nM 9.3 Antiproliferative activity against human Mino cells measured after 72 hrs by Cel... 31125896

Literature References

PubMed DOI Target Context # Activities
31125896 10.1016/j.ejmech.2019.05.035 ADMET 10
31125896 10.1016/j.ejmech.2019.05.035 Unchecked 1

Data from ChEMBL 36 via Core Engine