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Compound Detail

CHEMBL500815

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O=C(NS(=O)(=O)c1ccc(NCCSc2ccccc2)c([N+](=O)[O-])c1)c1ccc(N2CCN(Cc3ccccc3-c3ccc(Cl)cc3)CC2)cc1

Basic Information

ChEMBL ID CHEMBL500815
Phase Preclinical
Structure Type MOL
InChI Key RLJOZRFWOFYEQE-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
5
Publications
0
Known Names

Molecular Properties

742.3
MW (Da)
7.56
ALogP
9
HBA
2
HBD
124.9
PSA (Ų)
0.05
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 C38H36ClN5O5S2
MW 742.32
Aromatic Rings 5
Heavy Atoms 51
NP-Likeness -1.68

Activity Summary

EC50 1 meas. best 4.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NON-PROTEIN TARGET
CHEMBL3879801
EC50 4.48 4.48 33000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 7720.13 ng.hr.mL-1 Rattus norvegicus
Cmax 1150.0 nM Rattus norvegicus
F 28.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
NON-PROTEIN TARGET EC50 = 33000.0 nM 4.48 Cytotoxicity against human NCI-H146 cells assessed as cell viability after 48 hr... 18841882

Literature References

PubMed DOI Target Context # Activities
18841882 10.1021/jm800669s Rattus norvegicus 3
18841882 10.1021/jm800669s NON-PROTEIN TARGET 1
18841882 10.1021/jm800669s Unchecked 1
18841882 10.1021/jm800669s Bcl2-associated agonist of cell death 1
18841882 10.1021/jm800669s Apoptosis regulator Bcl-2 1

Data from ChEMBL 36 via Core Engine