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Compound Detail

CHEMBL3194086

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O=C1C=C(Nc2ccccc2C(=O)O)c2ccccc2C1=O

Basic Information

ChEMBL ID CHEMBL3194086
Phase Preclinical
Structure Type MOL
InChI Key DKNWWFXZRIJCFI-UHFFFAOYSA-N
10
Targets
15
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

293.3
MW (Da)
2.60
ALogP
4
HBA
2
HBD
83.5
PSA (Ų)
0.85
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H11NO4
MW 293.28
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness 0.18

Activity Summary

IC50 13 meas. best 5.72
EC50 2 meas. best 5.63

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
SUMO-activating enzyme
CHEMBL2095174
IC50 5.72 5.21 1900.0 2
Sentrin-specific protease 6
CHEMBL1741215
IC50 5.7 5.7 2000.0 1
Protein RecA
CHEMBL1741171
EC50 5.63 5.63 2340.0 1
Sentrin-specific protease 8
CHEMBL1741207
IC50 5.48 5.48 3300.0 1
Unchecked
CHEMBL612545
IC50 5.45 5.3167 3586.0 3
Apoptotic protease-activating factor 1
CHEMBL1795093
IC50 5.42 5.42 3840.0 1
Caspase-3
CHEMBL2334
IC50 5.32 5.32 4800.0 1
Tyrosyl-DNA phosphodiesterase 2
CHEMBL2169736
IC50 5.18 5.18 6561.0 1
Sentrin-specific protease 7
CHEMBL1741213
IC50 5.11 5.11 7860.0 1
Hexokinase HKDC1
CHEMBL1741200
IC50 4.91 4.84 12400.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
SUMO-activating enzyme IC50 = 1900.0 nM 5.72 PUBCHEM_BIOASSAY: AlphaScreen confirmatory assay for validation of inhibitors of... -
Sentrin-specific protease 6 IC50 = 2000.0 nM 5.7 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
Protein RecA EC50 = 2340.0 nM 5.63 PUBCHEM_BIOASSAY: Fluorescence Cell-Free Homogeneous Dose Retest to Identify Inh... -
Sentrin-specific protease 8 IC50 = 3300.0 nM 5.48 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
Unchecked IC50 = 3586.0 nM 5.45 PubChem BioAssay. Fluorescence-based biochemical high throughput screening dose ... -
Apoptotic protease-activating factor 1 IC50 = 3840.0 nM 5.42 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 in a Fluore... -
Unchecked IC50 = 4280.0 nM 5.37 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 using a LZ-... -
Caspase-3 IC50 = 4800.0 nM 5.32 PUBCHEM_BIOASSAY: Dose Response confirmation of inhibitors of Sentrin-specific p... -
Tyrosyl-DNA phosphodiesterase 2 IC50 = 6561.0 nM 5.18 PubChem BioAssay. Epi Absorbance-based biochemical high throughput dose response... -
Unchecked IC50 = 7386.0 nM 5.13 PubChem BioAssay. Counterscreen for inhibitors of Crimean-Congo Hemorrhagic Feve... -
Sentrin-specific protease 7 IC50 = 7860.0 nM 5.11 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
Hexokinase HKDC1 IC50 = 12400.0 nM 4.91 PUBCHEM_BIOASSAY: Dose Response confirmation of inhibitors of hexokinase domain ... -
Hexokinase HKDC1 IC50 = 16900.0 nM 4.77 PUBCHEM_BIOASSAY: Dose Response confirmation of inhibitors of hexokinase domain ... -
SUMO-activating enzyme IC50 = 19760.0 nM 4.7 PUBCHEM_BIOASSAY: uHTS HTRF assay for identification of inhibitors of SUMOylatio... -

Data from ChEMBL 36 via Core Engine