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Compound Detail

CHEMBL3195749

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COC(=O)c1ccccc1NC1=C/C(=N\S(=O)(=O)c2cccs2)c2ccccc2C1=O

Basic Information

ChEMBL ID CHEMBL3195749
Phase Preclinical
Structure Type MOL
InChI Key SQTXZQUPJDPRBX-HKOYGPOVSA-N
12
Targets
20
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

452.5
MW (Da)
3.91
ALogP
7
HBA
1
HBD
101.9
PSA (Ų)
0.59
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H16N2O5S2
MW 452.51
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.11

Activity Summary

IC50 16 meas. best 6.01
EC50 4 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein RecA
CHEMBL1741171
EC50 7.68 7.68 20.8 1
Unchecked
CHEMBL612545
IC50 6.01 5.684 980.0 5
Glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase
CHEMBL1741212
IC50 5.9 5.175 1260.0 2
Apoptotic protease-activating factor 1
CHEMBL1795093
IC50 5.74 5.74 1820.0 1
Sentrin-specific protease 6
CHEMBL1741215
IC50 5.73 5.73 1860.0 1
H4
CHEMBL1075452
EC50 5.72 5.72 1886.0 1
X-box-binding protein 1
CHEMBL1741176
IC50 5.44 5.44 3620.0 1
Unchecked
CHEMBL612545
EC50 5.1 5.095 7965.0 2
Glucose-6-phosphate 1-dehydrogenase
CHEMBL5347
IC50 4.57 4.57 27200.0 1
Hexokinase HKDC1
CHEMBL1741200
IC50 4.56 4.4 27500.0 2
Sentrin-specific protease 7
CHEMBL1741213
IC50 4.49 4.49 32330.0 1
Sentrin-specific protease 8
CHEMBL1741207
IC50 4.38 4.38 41200.0 1
Caspase-3
CHEMBL2334
IC50 4.17 4.17 68400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein RecA EC50 = 20.8 nM 7.68 PUBCHEM_BIOASSAY: Fluorescence Cell-Free Homogeneous Dose Retest to Identify Inh... -
Unchecked IC50 = 980.0 nM 6.01 PUBCHEM_BIOASSAY: Dose response cytotoxicity of uHTS chemical inhibitors of T-ce... -
Unchecked IC50 = 1040.0 nM 5.98 PUBCHEM_BIOASSAY: Dose response counterscreen of uHTS chemical inhibitors of T-c... -
Glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase IC50 = 1260.0 nM 5.9 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS small molecule inhibitors o... -
Apoptotic protease-activating factor 1 IC50 = 1820.0 nM 5.74 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 in a Fluore... -
Sentrin-specific protease 6 IC50 = 1860.0 nM 5.73 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
H4 EC50 = 1886.0 nM 5.72 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Activato... -
Unchecked IC50 = 2630.0 nM 5.58 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 using a LZ-... -
Unchecked IC50 = 2910.0 nM 5.54 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS chemical inhibitors of T-ce... -
X-box-binding protein 1 IC50 = 3620.0 nM 5.44 PUBCHEM_BIOASSAY: XBP1 DR counterscreen for CHOP. (Class of assay: confirmatory)... -
Unchecked IC50 = 4910.0 nM 5.31 PUBCHEM_BIOASSAY: Dose Response selectivity of uHTS chemical inhibitors of T-cel... -
Unchecked EC50 = 7965.0 nM 5.1 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Compounds that Suppress the... -
Unchecked EC50 = 8185.0 nM 5.09 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Compounds that Suppress the... -
Glucose-6-phosphate 1-dehydrogenase IC50 = 27200.0 nM 4.57 PUBCHEM_BIOASSAY: Human Glucose-6-Phosphate Dehydrogenase Dose Response Selectiv... -
Hexokinase HKDC1 IC50 = 27500.0 nM 4.56 PUBCHEM_BIOASSAY: Dose Response confirmation of inhibitors of hexokinase domain ... -
Sentrin-specific protease 7 IC50 = 32330.0 nM 4.49 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
Glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase IC50 = 35700.0 nM 4.45 PUBCHEM_BIOASSAY: Dose Response orthogonal kinetic assay utilizing the direct de... -
Sentrin-specific protease 8 IC50 = 41200.0 nM 4.38 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
Hexokinase HKDC1 IC50 = 57000.0 nM 4.24 PUBCHEM_BIOASSAY: Dose Response confirmation of inhibitors of hexokinase domain ... -
Caspase-3 IC50 = 68400.0 nM 4.17 PUBCHEM_BIOASSAY: Dose Response confirmation of inhibitors of Sentrin-specific p... -

Data from ChEMBL 36 via Core Engine