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Compound Detail

CHEMBL1454614

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O=C1C=C(N2CCOCC2)c2ccccc2C1=O

Basic Information

ChEMBL ID CHEMBL1454614
Phase Preclinical
Structure Type MOL
InChI Key CGVPOLUKPMAOAN-UHFFFAOYSA-N
8
Targets
20
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

243.3
MW (Da)
1.13
ALogP
4
HBA
0
HBD
46.6
PSA (Ų)
0.69
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H13NO3
MW 243.26
Aromatic Rings 1
Heavy Atoms 18
NP-Likeness -0.03

Activity Summary

IC50 14 meas. best 5.99
EC50 6 meas. best 6.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein RecA
CHEMBL1741171
EC50 6.82 6.82 150.0 1
Hexokinase HKDC1
CHEMBL1741200
IC50 5.99 5.945 1020.0 2
Apoptotic protease-activating factor 1
CHEMBL1795093
IC50 5.9 5.9 1270.0 1
Unchecked
CHEMBL612545
IC50 5.82 4.805 1530.0 6
Tyrosyl-DNA phosphodiesterase 2
CHEMBL2169736
IC50 5.59 5.59 2546.0 1
Unchecked
CHEMBL612545
EC50 5.16 5.1067 6880.0 3
Cysteine protease ATG4B
CHEMBL1741221
IC50 5.15 5.15 7070.0 1
HEK293
CHEMBL614818
EC50 5.06 5.06 8787.0 1
HEK293
CHEMBL614818
IC50 5.02 4.96 9463.5 3
Nucleotide-binding oligomerization domain-containing protein 2
CHEMBL1293266
EC50 4.88 4.88 13300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein RecA EC50 = 150.0 nM 6.82 PUBCHEM_BIOASSAY: Fluorescence Cell-Free Homogeneous Dose Retest to Identify Inh... -
Hexokinase HKDC1 IC50 = 1020.0 nM 5.99 PUBCHEM_BIOASSAY: Dose Response confirmation of inhibitors of hexokinase domain ... -
Apoptotic protease-activating factor 1 IC50 = 1270.0 nM 5.9 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 in a Fluore... -
Hexokinase HKDC1 IC50 = 1270.0 nM 5.9 PUBCHEM_BIOASSAY: Dose Response confirmation of inhibitors of hexokinase domain ... -
Unchecked IC50 = 1530.0 nM 5.82 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 using a LZ-... -
Tyrosyl-DNA phosphodiesterase 2 IC50 = 2546.0 nM 5.59 PubChem BioAssay. Epi Absorbance-based biochemical high throughput dose response... -
Unchecked IC50 = 4215.0 nM 5.38 PubChem BioAssay. Fluorescence-based biochemical high throughput screening dose ... -
Unchecked EC50 = 6880.0 nM 5.16 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Cysteine protease ATG4B IC50 = 7070.0 nM 5.15 PUBCHEM_BIOASSAY: Dose response confirmation of the uHTS fluorescent assay for i... -
Unchecked EC50 = 8407.0 nM 5.08 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhi... -
Unchecked EC50 = 8368.0 nM 5.08 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
HEK293 EC50 = 8787.0 nM 5.06 PUBCHEM_BIOASSAY: uHTS luminescence assay for the identification of compounds th... -
HEK293 IC50 = 9463.5 nM 5.02 PUBCHEM_BIOASSAY: HTS dose response assay for identification of inhibitors of TN... -
HEK293 IC50 = 10320.0 nM 4.99 PUBCHEM_BIOASSAY: uHTS luminescence assay for the identification of compounds th... -
Unchecked IC50 = 11931.0 nM 4.92 PubChem BioAssay. Counterscreen for inhibitors of Crimean-Congo Hemorrhagic Feve... -
Nucleotide-binding oligomerization domain-containing protein 2 EC50 = 13300.0 nM 4.88 PUBCHEM_BIOASSAY: uHTS luminescence assay for the identification of compounds th... -
HEK293 IC50 = 13559.86 nM 4.87 PUBCHEM_BIOASSAY: uHTS Fluorescence assay for the identification of cytotoxic co... -
Unchecked IC50 = 51240.0 nM 4.29 PUBCHEM_BIOASSAY: A small molecule screen for inhibitors of the PhoP region in S... -
Unchecked IC50 = 55470.0 nM 4.26 PUBCHEM_BIOASSAY: A Counter Screen to identiry small molecule screen for inhibit... -
Unchecked IC50 = 69920.0 nM 4.16 PUBCHEM_BIOASSAY: A screen for inhibitors of the PhoP region in Salmonella Typhi... -

Data from ChEMBL 36 via Core Engine