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Compound Detail

CHEMBL3189714

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Cc1ccccc1NC1=C/C(=N\S(=O)(=O)c2cccs2)c2ccccc2C1=O

Basic Information

ChEMBL ID CHEMBL3189714
Phase Preclinical
Structure Type MOL
InChI Key DBVTXTMIOWGNNH-PTGBLXJZSA-N
9
Targets
21
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 -1.34

Activity Summary

IC50 14 meas. best 6.61
EC50 7 meas. best 6.61

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 6.61 6.1 244.0 3
Unchecked
CHEMBL612545
IC50 6.61 5.761 248.6 10
Apoptotic protease-activating factor 1
CHEMBL1795093
IC50 6.47 6.47 335.0 1
Heat shock protein HSP 90-alpha
CHEMBL3880
IC50 6.36 6.36 437.6 1
Protein RecA
CHEMBL1741171
EC50 6.18 6.18 654.0 1
Streptococcus sp. 'group A'
CHEMBL612389
EC50 6.15 6.15 701.0 1
Streptokinase A
CHEMBL1293228
EC50 5.84 5.84 1435.0 1
Serine/threonine-protein phosphatase
CHEMBL1293265
IC50 5.74 5.74 1832.0 1
Streptococcus
CHEMBL612313
EC50 5.34 5.34 4554.0 1
Nuclear receptor coactivator 3
CHEMBL1293301
IC50 4.79 4.79 16400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 244.0 nM 6.61 PubChem BioAssay. Leishmania major promastigote EC50 determinations. (Class of... -
Unchecked IC50 = 248.56 nM 6.61 PubChem BioAssay. Fluorescence-based biochemical high throughput screening dose ... -
Apoptotic protease-activating factor 1 IC50 = 335.0 nM 6.47 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 in a Fluore... -
Unchecked IC50 = 410.0 nM 6.39 PUBCHEM_BIOASSAY: Dose response counterscreen of uHTS chemical inhibitors of T-c... -
Unchecked IC50 = 440.0 nM 6.36 PUBCHEM_BIOASSAY: Dose response cytotoxicity of uHTS chemical inhibitors of T-ce... -
Heat shock protein HSP 90-alpha IC50 = 437.61 nM 6.36 PUBCHEM_BIOASSAY: Luminescence-based dose response biochemical high throughput s... -
Unchecked IC50 = 548.0 nM 6.26 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 using a LZ-... -
Protein RecA EC50 = 654.0 nM 6.18 PUBCHEM_BIOASSAY: Fluorescence Cell-Free Homogeneous Dose Retest to Identify Inh... -
Streptococcus sp. 'group A' EC50 = 701.0 nM 6.15 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Unchecked EC50 = 1042.0 nM 5.98 PUBCHEM_BIOASSAY: Luminescence Cell-Based/Microorganism Dose Confirmation HTS to... -
Unchecked IC50 = 1043.0 nM 5.98 PubChem BioAssay. Counterscreen for inhibitors of Crimean-Congo Hemorrhagic Feve... -
Unchecked IC50 = 1250.0 nM 5.9 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS chemical inhibitors of T-ce... -
Streptokinase A EC50 = 1435.0 nM 5.84 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Serine/threonine-protein phosphatase IC50 = 1832.0 nM 5.74 PUBCHEM_BIOASSAY: Fluorescence-based biochemical high throughput dose response a... -
Unchecked EC50 = 1951.0 nM 5.71 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS Screen to Identify C... -
Streptococcus EC50 = 4554.0 nM 5.34 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... -
Unchecked IC50 = 6690.0 nM 5.17 PUBCHEM_BIOASSAY: Dose Response selectivity of uHTS chemical inhibitors of T-cel... -
Unchecked IC50 = 7970.0 nM 5.1 PUBCHEM_BIOASSAY: High Throughput Screening Assay used to Identify Novel Compoun... -
Unchecked IC50 = 11280.0 nM 4.95 PUBCHEM_BIOASSAY: A High Throughput Confirmatory Assay used to Identify Novel Co... -
Unchecked IC50 = 12980.0 nM 4.89 PUBCHEM_BIOASSAY: uHTS fluorescence for the identification of compounds that dec... -

Data from ChEMBL 36 via Core Engine