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Compound Detail

CHEMBL376254

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CN(C)CC[C@H](CSc1ccccc1)Nc1ccc(S(=O)(=O)NC(=O)c2ccc(N3CCC(=Cc4ccccc4C(F)(F)F)CC3)cc2)cc1[N+](=O)[O-]

Basic Information

ChEMBL ID CHEMBL376254
Phase Preclinical
Structure Type MOL
InChI Key RSGYTDGOUIXVMA-SSEXGKCCSA-N
2
Targets
4
Activities
3
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

767.9
MW (Da)
7.94
ALogP
9
HBA
2
HBD
124.9
PSA (Ų)
0.07
QED
2
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C38H40F3N5O5S2
MW 767.90
Aromatic Rings 4
Heavy Atoms 53
NP-Likeness -1.37

Activity Summary

EC50 2 meas. best 6.82
IC50 1 meas. best 6.52
Ki 1 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Apoptosis regulator Bcl-2
CHEMBL4860
Ki 8.7 8.7 2.0 1
Bcl-2-like protein 1
CHEMBL4625
EC50 6.82 6.82 150.0 1
Apoptosis regulator Bcl-2
CHEMBL4860
EC50 6.68 6.68 210.0 1
Bcl-2-like protein 1
CHEMBL4625
IC50 6.52 6.52 300.0 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