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Compound Detail

CHEMBL175434

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NS(=O)(=O)c1ccc(NC2=CC(=O)C(=O)c3ccccc32)cc1

Basic Information

ChEMBL ID CHEMBL175434
Phase Preclinical
Structure Type MOL
InChI Key DIHFBNUDSJVTRQ-UHFFFAOYSA-N
11
Targets
16
Activities
3
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

328.4
MW (Da)
1.55
ALogP
5
HBA
2
HBD
106.3
PSA (Ų)
0.83
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 C16H12N2O4S
MW 328.35
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -0.41

Activity Summary

IC50 12 meas. best 5.68
EC50 3 meas. best 6.18
Ki 1 meas. best 4.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein RecA
CHEMBL1741171
EC50 6.18 6.18 667.0 1
Apoptotic protease-activating factor 1
CHEMBL1795093
IC50 5.68 5.68 2080.0 1
SUMO-activating enzyme
CHEMBL2095174
IC50 5.68 5.35 2110.0 2
Sentrin-specific protease 6
CHEMBL1741215
IC50 5.54 5.54 2890.0 1
Unchecked
CHEMBL612545
IC50 5.31 5.1733 4852.0 3
Sentrin-specific protease 8
CHEMBL1741207
IC50 5.3 5.3 4960.0 1
Tyrosyl-DNA phosphodiesterase 2
CHEMBL2169736
IC50 5.25 5.25 5588.0 1
Sentrin-specific protease 7
CHEMBL1741213
IC50 5.1 5.1 7930.0 1
Unchecked
CHEMBL612545
EC50 5.07 4.84 8454.0 2
Caspase-3
CHEMBL2334
IC50 5.01 5.01 9750.0 1
Serine/threonine-protein phosphatase PP1-alpha catalytic subunit
CHEMBL2164
IC50 4.41 4.41 38859.0 1
Macrophage migration inhibitory factor homologue
CHEMBL2176864
Ki 4.0 4.0 99000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein RecA EC50 = 667.0 nM 6.18 PUBCHEM_BIOASSAY: Fluorescence Cell-Free Homogeneous Dose Retest to Identify Inh... -
SUMO-activating enzyme IC50 = 2110.0 nM 5.68 PUBCHEM_BIOASSAY: AlphaScreen confirmatory assay for validation of inhibitors of... -
Apoptotic protease-activating factor 1 IC50 = 2080.0 nM 5.68 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 in a Fluore... -
Sentrin-specific protease 6 IC50 = 2890.0 nM 5.54 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
Unchecked IC50 = 4852.0 nM 5.31 PubChem BioAssay. Fluorescence-based biochemical high throughput screening dose ... -
Sentrin-specific protease 8 IC50 = 4960.0 nM 5.3 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
Unchecked IC50 = 5360.0 nM 5.27 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 using a LZ-... -
Tyrosyl-DNA phosphodiesterase 2 IC50 = 5588.0 nM 5.25 PubChem BioAssay. Epi Absorbance-based biochemical high throughput dose response... -
Sentrin-specific protease 7 IC50 = 7930.0 nM 5.1 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
Unchecked EC50 = 8454.0 nM 5.07 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhi... -
SUMO-activating enzyme IC50 = 9540.0 nM 5.02 PUBCHEM_BIOASSAY: uHTS HTRF assay for identification of inhibitors of SUMOylatio... -
Caspase-3 IC50 = 9750.0 nM 5.01 PUBCHEM_BIOASSAY: Dose Response confirmation of inhibitors of Sentrin-specific p... -
Unchecked IC50 = 11511.0 nM 4.94 PubChem BioAssay. Counterscreen for inhibitors of Crimean-Congo Hemorrhagic Feve... -
Unchecked EC50 = 24359.0 nM 4.61 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
Serine/threonine-protein phosphatase PP1-alpha catalytic subunit IC50 = 38859.0 nM 4.41 PUBCHEM_BIOASSAY: Counterscreen for inhibitors of PP5: fluorescence-based bioche... -
Macrophage migration inhibitory factor homologue Ki = 99000.0 nM 4.0 Inhibition of recombinant Plasmodium falciparum MIF expressed in Escherichia col... 23067344

Literature References

PubMed DOI Target Context # Activities
15715473 10.1021/jm049332v Prostaglandin G/H synthase 2 1
15715473 10.1021/jm049332v Prostaglandin G/H synthase 1 1
23067344 10.1021/jm301269s Macrophage migration inhibitory factor homologue 1

Data from ChEMBL 36 via Core Engine