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Compound Detail

CHEMBL221294

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COC1(Cc2ccccc2-c2ccccc2)CCN(c2ccc(C(=O)NS(=O)(=O)c3ccc(N[C@H](CCN(C)C)CSc4ccccc4)c([N+](=O)[O-])c3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL221294
Phase Preclinical
Structure Type MOL
InChI Key GOUUFVVBOJUOIM-PSXMRANNSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

808.0
MW (Da)
8.13
ALogP
10
HBA
2
HBD
134.1
PSA (Ų)
0.05
QED
2
Ro5 Violations
17
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C44H49N5O6S2
MW 808.04
Aromatic Rings 5
Heavy Atoms 57
NP-Likeness -0.94

Activity Summary

EC50 2 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Apoptosis regulator Bcl-2
CHEMBL4860
EC50 7.7 7.7 20.0 1
Bcl-2-like protein 1
CHEMBL4625
EC50 7.46 7.46 35.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17256834 10.1021/jm061152t Bcl-2-like protein 1 3
17256834 10.1021/jm061152t Apoptosis regulator Bcl-2 2

Data from ChEMBL 36 via Core Engine