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Compound Detail

CHEMBL1999630

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Cc1ccccc1NC1=C/C(=N\S(=O)(=O)c2ccc(C(=O)O)cc2)c2ccccc2C1=O

Basic Information

ChEMBL ID CHEMBL1999630
Phase Preclinical
Structure Type MOL
InChI Key QMMIFWYVGNVUCF-YYADALCUSA-N
13
Targets
17
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

446.5
MW (Da)
4.06
ALogP
5
HBA
2
HBD
112.9
PSA (Ų)
0.61
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 C24H18N2O5S
MW 446.48
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.83

Activity Summary

IC50 12 meas. best 6.59
EC50 5 meas. best 5.78

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.59 5.65 256.7 4
Heat shock protein HSP 90-alpha
CHEMBL3880
IC50 6.28 6.28 521.6 1
Tyrosyl-DNA phosphodiesterase 2
CHEMBL2169736
IC50 5.85 5.85 1411.0 1
Apoptotic protease-activating factor 1
CHEMBL1795093
IC50 5.8 5.8 1590.0 1
Streptococcus sp. 'group A'
CHEMBL612389
EC50 5.78 5.78 1674.0 1
Streptokinase A
CHEMBL1293228
EC50 5.72 5.72 1897.0 1
Hexokinase HKDC1
CHEMBL1741200
IC50 5.6 5.575 2530.0 2
Protein RecA
CHEMBL1741171
EC50 5.43 5.43 3670.0 1
Streptococcus
CHEMBL612313
EC50 5.3 5.3 5012.0 1
Cysteine protease ATG4B
CHEMBL1741221
IC50 5.23 5.23 5850.0 1
Potassium voltage-gated channel subfamily KQT member 2
CHEMBL5530
EC50 5.02 5.02 9510.0 1
Phospholipase A2
CHEMBL4426
IC50 4.81 4.81 15400.0 1
1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1
CHEMBL3964
IC50 4.04 4.04 90069.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 256.73 nM 6.59 PubChem BioAssay. Fluorescence-based biochemical high throughput screening dose ... -
Heat shock protein HSP 90-alpha IC50 = 521.6 nM 6.28 PUBCHEM_BIOASSAY: Luminescence-based dose response biochemical high throughput s... -
Unchecked IC50 = 535.73 nM 6.27 PubChem BioAssay. Counterscreen for inhibitors of Crimean-Congo Hemorrhagic Feve... -
Tyrosyl-DNA phosphodiesterase 2 IC50 = 1411.0 nM 5.85 PubChem BioAssay. Epi Absorbance-based biochemical high throughput dose response... -
Apoptotic protease-activating factor 1 IC50 = 1590.0 nM 5.8 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 in a Fluore... -
Streptococcus sp. 'group A' EC50 = 1674.0 nM 5.78 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptokinase A EC50 = 1897.0 nM 5.72 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Hexokinase HKDC1 IC50 = 2530.0 nM 5.6 PUBCHEM_BIOASSAY: Dose Response confirmation of inhibitors of hexokinase domain ... -
Hexokinase HKDC1 IC50 = 2840.0 nM 5.55 PUBCHEM_BIOASSAY: Dose Response confirmation of inhibitors of hexokinase domain ... -
Unchecked IC50 = 3080.0 nM 5.51 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 using a LZ-... -
Protein RecA EC50 = 3670.0 nM 5.43 PUBCHEM_BIOASSAY: Fluorescence Cell-Free Homogeneous Dose Retest to Identify Inh... -
Streptococcus EC50 = 5012.0 nM 5.3 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... -
Cysteine protease ATG4B IC50 = 5850.0 nM 5.23 PUBCHEM_BIOASSAY: Dose response confirmation of the uHTS fluorescent assay for i... -
Potassium voltage-gated channel subfamily KQT member 2 EC50 = 9510.0 nM 5.02 PUBCHEM_BIOASSAY: Mode of action assay-Automated electrophysiology assay of comp... -
Phospholipase A2 IC50 = 15400.0 nM 4.81 PUBCHEM_BIOASSAY: Dose response counterscreen of uHTS hits for ATG4B inhibitors ... -
Unchecked IC50 = 58500.0 nM 4.23 PUBCHEM_BIOASSAY: Luminescence-based counterscreen assay for HSP90 inhibitors: d... -
1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1 IC50 = 90069.0 nM 4.04 PubChem BioAssay. Counterscreen for inhibitors of phospholipase C isozymes (PLC-... -

Data from ChEMBL 36 via Core Engine