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Compound Detail

CHEMBL286404

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COC(=O)c1[nH]c2ccccc2c1Sc1ccccc1

Basic Information

ChEMBL ID CHEMBL286404
Phase Preclinical
Structure Type MOL
InChI Key ZFFZRQNMJVPVBG-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

283.4
MW (Da)
4.11
ALogP
3
HBA
1
HBD
42.1
PSA (Ų)
0.74
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H13NO2S
MW 283.35
Aromatic Rings 3
Heavy Atoms 20
NP-Likeness -0.69

Activity Summary

IC50 2 meas. best 5.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
IC50 5.6 5.6 2500.0 1
Tubulin
CHEMBL2095182
IC50 5.08 5.08 8300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Human immunodeficiency virus type 1 protease IC50 = 2500.0 nM 5.6 Inhibition of HIV-1 RT using rC-dG as template 7683725
Tubulin IC50 = 8300.0 nM 5.08 Inhibition of tubulin polymerization 15566282

Literature References

PubMed DOI Target Context # Activities
15566282 10.1021/jm049360d Tubulin 2
7683725 10.1021/jm00061a022 Human immunodeficiency virus type 1 protease 1
7683725 10.1021/jm00061a022 MT4 1
15566282 10.1021/jm049360d MCF7 1

Data from ChEMBL 36 via Core Engine