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Compound Detail

CHEMBL1369492

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CCc1nnc(NS(=O)(=O)c2ccc(NC(=S)NC(=O)/C=C/c3ccc(C(C)C)cc3)cc2)s1

Basic Information

ChEMBL ID CHEMBL1369492
Phase Preclinical
Structure Type MOL
InChI Key IMLRWXNCJUEBEP-VGOFMYFVSA-N
12
Targets
14
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

515.7
MW (Da)
4.55
ALogP
7
HBA
3
HBD
113.1
PSA (Ų)
0.30
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25N5O3S3
MW 515.69
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -2.01

Activity Summary

IC50 9 meas. best 5.8
EC50 5 meas. best 5.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
G-protein coupled receptor 35
CHEMBL1293267
IC50 5.8 5.8 1593.4 1
Streptococcus sp. 'group A'
CHEMBL612389
EC50 5.62 5.62 2386.0 1
Streptokinase A
CHEMBL1293228
EC50 5.51 5.43 3108.0 2
Tyrosine-protein phosphatase non-receptor type 7
CHEMBL2219
IC50 5.22 5.22 5990.0 1
DNA (cytosine-5)-methyltransferase 1
CHEMBL1993
IC50 5.21 5.21 6160.0 1
Streptococcus
CHEMBL612313
EC50 5.11 5.11 7830.0 1
Plectin
CHEMBL1293240
IC50 5.05 4.885 8871.0 2
X-box-binding protein 1
CHEMBL1741176
IC50 5.0 5.0 10000.0 1
DNA damage-inducible transcript 3 protein
CHEMBL2146304
IC50 5.0 5.0 10000.0 1
Envelope glycoprotein gp160
CHEMBL1293311
IC50 4.92 4.92 12100.0 1
Dual specificity protein phosphatase 3
CHEMBL2635
IC50 4.82 4.82 15000.0 1
Protein RecA
CHEMBL1741171
EC50 4.48 4.48 33400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
G-protein coupled receptor 35 IC50 = 1593.44 nM 5.8 PUBCHEM_BIOASSAY: Image-Based HTS for Selective Antagonists of GPR35. High conte... -
Streptococcus sp. 'group A' EC50 = 2386.0 nM 5.62 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptokinase A EC50 = 3108.0 nM 5.51 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptokinase A EC50 = 4441.0 nM 5.35 PUBCHEM_BIOASSAY: Absorbance Microorganism-Based Dose Response HTS to Identify I... -
Tyrosine-protein phosphatase non-receptor type 7 IC50 = 5990.0 nM 5.22 PUBCHEM_BIOASSAY: SAR analysis of chemical inhibitors of HePTP using a Fluoresce... -
DNA (cytosine-5)-methyltransferase 1 IC50 = 6160.0 nM 5.21 PUBCHEM_BIOASSAY: Dose response confirmation of DNMT1 inhibitors in a Fluorescen... -
Streptococcus EC50 = 7830.0 nM 5.11 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... -
Plectin IC50 = 8871.0 nM 5.05 PUBCHEM_BIOASSAY: HTS TR-FRET-based dose response confirmatory assay for Siah-1.... -
X-box-binding protein 1 IC50 = 10000.0 nM 5.0 PUBCHEM_BIOASSAY: XBP1 DR counterscreen for CHOP. (Class of assay: confirmatory)... -
DNA damage-inducible transcript 3 protein IC50 = 10000.0 nM 5.0 PUBCHEM_BIOASSAY: CHOP dose-response primary assay. (Class of assay: confirmator... -
Envelope glycoprotein gp160 IC50 = 12100.0 nM 4.92 PUBCHEM_BIOASSAY: uHTS fluorescence assay for the identification of Human Immuno... -
Dual specificity protein phosphatase 3 IC50 = 15000.0 nM 4.82 PUBCHEM_BIOASSAY: SAR VHR1 Fluorescent Assay for In Vitro dose response studies ... -
Plectin IC50 = 19164.0 nM 4.72 PUBCHEM_BIOASSAY: uHTS identification of small molecule antagonists of the bindi... -
Protein RecA EC50 = 33400.0 nM 4.48 PUBCHEM_BIOASSAY: Fluorescence Cell-Free Homogeneous Dose Retest to Identify Inh... -

Data from ChEMBL 36 via Core Engine