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Compound Detail

CHEMBL382361

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COc1cc(CC(=O)N(C)C)ccc1-c1ccc(C(=O)NS(=O)(=O)c2ccc(NCCSc3ccccc3)c([N+](=O)[O-])c2)cc1

Basic Information

ChEMBL ID CHEMBL382361
Phase Preclinical
Structure Type MOL
InChI Key HVJXFZCZZCTBLU-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

648.8
MW (Da)
5.22
ALogP
9
HBA
2
HBD
147.9
PSA (Ų)
0.09
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H32N4O7S2
MW 648.76
Aromatic Rings 4
Heavy Atoms 45
NP-Likeness -1.46

Activity Summary

Ki 1 meas. best 6.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bcl-2-like protein 1
CHEMBL4625
Ki 6.6 6.6 251.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Bcl-2-like protein 1 Ki = 251.0 nM 6.6 Binding affinity to Bcl-XL by fluorescence polarization assay 16451081

Literature References

PubMed DOI Target Context # Activities
16451081 10.1021/jm050754u Bcl-2-like protein 1 2
16451081 10.1021/jm050754u Apoptosis regulator Bcl-2 1

Data from ChEMBL 36 via Core Engine