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Compound Detail

CHEMBL3196451

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Cc1ccc(NC2=C/C(=N/S(=O)(=O)c3cccs3)c3ccccc3C2=O)cc1

Basic Information

ChEMBL ID CHEMBL3196451
Phase Preclinical
Structure Type MOL
InChI Key XYTTUUGZACDZAR-NKFKGCMQSA-N
9
Targets
13
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

408.5
MW (Da)
4.43
ALogP
5
HBA
1
HBD
75.6
PSA (Ų)
0.69
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H16N2O3S2
MW 408.50
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.29

Activity Summary

IC50 10 meas. best 6.73
EC50 3 meas. best 6.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein RecA
CHEMBL1741171
EC50 6.92 6.92 119.0 1
Sentrin-specific protease 6
CHEMBL1741215
IC50 6.73 6.73 186.0 1
Sentrin-specific protease 8
CHEMBL1741207
IC50 6.61 6.61 244.0 1
Sentrin-specific protease 7
CHEMBL1741213
IC50 6.45 6.45 359.0 1
Unchecked
CHEMBL612545
IC50 6.39 6.0667 405.1 3
Apoptotic protease-activating factor 1
CHEMBL1795093
IC50 6.34 6.34 453.0 1
Caspase-3
CHEMBL2334
IC50 5.68 5.68 2100.0 1
Unchecked
CHEMBL612545
EC50 5.55 5.5 2823.0 2
Tyrosyl-DNA phosphodiesterase 2
CHEMBL2169736
IC50 5.48 5.48 3297.0 1
Beta-galactosidase
CHEMBL1293264
IC50 4.29 4.29 50800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein RecA EC50 = 119.0 nM 6.92 PUBCHEM_BIOASSAY: Fluorescence Cell-Free Homogeneous Dose Retest to Identify Inh... -
Sentrin-specific protease 6 IC50 = 186.0 nM 6.73 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
Sentrin-specific protease 8 IC50 = 244.0 nM 6.61 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
Sentrin-specific protease 7 IC50 = 359.0 nM 6.45 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
Unchecked IC50 = 405.13 nM 6.39 PubChem BioAssay. Fluorescence-based biochemical high throughput screening dose ... -
Apoptotic protease-activating factor 1 IC50 = 453.0 nM 6.34 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 in a Fluore... -
Unchecked IC50 = 869.0 nM 6.06 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 using a LZ-... -
Unchecked IC50 = 1792.0 nM 5.75 PubChem BioAssay. Counterscreen for inhibitors of Crimean-Congo Hemorrhagic Feve... -
Caspase-3 IC50 = 2100.0 nM 5.68 PUBCHEM_BIOASSAY: Dose Response confirmation of inhibitors of Sentrin-specific p... -
Unchecked EC50 = 2823.0 nM 5.55 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Compounds that Suppress the... -
Tyrosyl-DNA phosphodiesterase 2 IC50 = 3297.0 nM 5.48 PubChem BioAssay. Epi Absorbance-based biochemical high throughput dose response... -
Unchecked EC50 = 3562.0 nM 5.45 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Compounds that Suppress the... -
Beta-galactosidase IC50 = 50800.0 nM 4.29 PUBCHEM_BIOASSAY: HTS Dose response counterscreen for assays utilizing the enzym... -

Data from ChEMBL 36 via Core Engine