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Compound Detail

CHEMBL1405964

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CCCCn1c(NS(=O)(=O)c2ccccc2)c(S(=O)(=O)c2ccc(C)cc2)c2nc3ccccc3nc21

Basic Information

ChEMBL ID CHEMBL1405964
Phase Preclinical
Structure Type MOL
InChI Key GCZZEBZXVDWJBN-UHFFFAOYSA-N
10
Targets
16
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

534.7
MW (Da)
5.33
ALogP
7
HBA
1
HBD
111.0
PSA (Ų)
0.29
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H26N4O4S2
MW 534.66
Aromatic Rings 5
Heavy Atoms 37
NP-Likeness -1.37

Activity Summary

IC50 10 meas. best 6.3
EC50 6 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein RecA
CHEMBL1741171
EC50 7.1 7.1 80.1 1
SUMO-activating enzyme
CHEMBL2095174
IC50 6.3 6.07 500.0 3
Plectin
CHEMBL1293240
IC50 5.8 5.8 1599.9 1
Streptokinase A
CHEMBL1293228
EC50 5.46 5.1 3433.0 2
Streptococcus sp. 'group A'
CHEMBL612389
EC50 5.45 5.45 3564.0 1
SUMO E1/E2
CHEMBL3137290
IC50 5.38 5.38 4200.0 1
Unchecked
CHEMBL612545
IC50 5.22 5.125 5990.0 2
Tyrosyl-DNA phosphodiesterase 2
CHEMBL2169736
IC50 5.11 5.11 7833.0 1
X-box-binding protein 1
CHEMBL1741176
IC50 5.0 5.0 10000.0 1
Unchecked
CHEMBL612545
EC50 4.92 4.92 12020.0 1
Streptococcus
CHEMBL612313
EC50 4.85 4.85 14144.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein RecA EC50 = 80.1 nM 7.1 PUBCHEM_BIOASSAY: Fluorescence Cell-Free Homogeneous Dose Retest to Identify Inh... -
SUMO-activating enzyme IC50 = 500.0 nM 6.3 Biochemical Assay: Through the Molecular Library Probe Production Center Network... -
SUMO-activating enzyme IC50 = 680.0 nM 6.17 PUBCHEM_BIOASSAY: AlphaScreen confirmatory assay for validation of inhibitors of... -
Plectin IC50 = 1599.87 nM 5.8 PUBCHEM_BIOASSAY: HTS TR-FRET-based dose response confirmatory assay for Siah-1.... -
SUMO-activating enzyme IC50 = 1830.0 nM 5.74 PUBCHEM_BIOASSAY: uHTS HTRF assay for identification of inhibitors of SUMOylatio... -
Streptokinase A EC50 = 3433.0 nM 5.46 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptococcus sp. 'group A' EC50 = 3564.0 nM 5.45 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
SUMO E1/E2 IC50 = 4200.0 nM 5.38 PUBCHEM_BIOASSAY: SAR analysis of SUMOylation using HTRF in an in-Vitro dose res... -
Unchecked IC50 = 5990.0 nM 5.22 PUBCHEM_BIOASSAY: A small molecule screen for inhibitors of the PhoP region in S... -
Tyrosyl-DNA phosphodiesterase 2 IC50 = 7833.0 nM 5.11 PubChem BioAssay. Epi Absorbance-based biochemical high throughput dose response... -
Unchecked IC50 = 9390.0 nM 5.03 PUBCHEM_BIOASSAY: A counter screen for small molecule screen for inhibitors of t... -
X-box-binding protein 1 IC50 = 10000.0 nM 5.0 PUBCHEM_BIOASSAY: XBP1 DR counterscreen for CHOP. (Class of assay: confirmatory)... -
Unchecked EC50 = 12020.0 nM 4.92 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Streptococcus EC50 = 14144.0 nM 4.85 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... -
Streptokinase A EC50 = 18250.0 nM 4.74 PUBCHEM_BIOASSAY: Absorbance Microorganism-Based Dose Response HTS to Identify I... -

Data from ChEMBL 36 via Core Engine