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Compound Detail

CHEMBL3094228

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O=C1C(=O)C(Nc2ccncc2)C1NCCCCCCS(=O)(=O)N(OCCN1CCOCC1)C1CCCCC1

Basic Information

ChEMBL ID CHEMBL3094228
Phase Preclinical
Structure Type MOL
InChI Key GHPFJFIFYMTOFD-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
6
PK Parameters
4
Publications
0
Known Names

Molecular Properties

565.7
MW (Da)
1.76
ALogP
10
HBA
2
HBD
130.2
PSA (Ų)
0.17
QED
1
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H43N5O6S
MW 565.74
Aromatic Rings 1
Heavy Atoms 39
NP-Likeness -0.70

Activity Summary

IC50 3 meas. best 9.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
A2780
CHEMBL614004
IC50 9.31 9.31 0.5 1
MCF7
CHEMBL387
IC50 8.05 8.05 9.0 1
HCT-116
CHEMBL394
IC50 7.41 7.41 39.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 12499.0 ng.hr.mL-1 Mus musculus
CL 66.58 mL.min-1.kg-1 Mus musculus
Cmax 59285.18 nM Mus musculus
T1/2 0.21 hr Mus musculus
Tmax 0.083 hr Mus musculus
Vd 1.2 L.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24164086 10.1021/jm4009949 Mus musculus 8
24164086 10.1021/jm4009949 HCT-116 3
24164086 10.1021/jm4009949 MCF7 1
24164086 10.1021/jm4009949 A2780 1

Data from ChEMBL 36 via Core Engine