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Compound Detail

CHEMBL1318943

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[O-][N+]1=c2ccc(Nc3ccccc3)cc2=NC12CCCCC2

Basic Information

ChEMBL ID CHEMBL1318943
Phase Preclinical
Structure Type MOL
InChI Key QEKYDTGXFOVMRB-UHFFFAOYSA-N
7
Targets
12
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

293.4
MW (Da)
2.71
ALogP
3
HBA
1
HBD
50.5
PSA (Ų)
0.68
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H19N3O
MW 293.37
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -0.29

Activity Summary

EC50 9 meas. best 6.12
IC50 3 meas. best 6.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.2 6.2 637.0 1
ATP-dependent molecular chaperone HSP82
CHEMBL1293251
EC50 6.12 6.12 750.0 1
Unchecked
CHEMBL612545
EC50 6.03 5.8425 942.0 4
Protein RecA
CHEMBL1741171
EC50 5.36 5.36 4370.0 1
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 5.28 5.28 5197.0 1
Peroxisome proliferator-activated receptor gamma/Nuclear receptor coactivator 2
CHEMBL2095163
EC50 4.84 4.84 14390.0 1
Peroxisome proliferator-activated receptor gamma/Nuclear receptor coactivator 1
CHEMBL2095162
EC50 4.83 4.83 14900.0 1
Mannose-6-phosphate isomerase
CHEMBL2758
IC50 4.32 4.32 48238.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 637.0 nM 6.2 PUBCHEM_BIOASSAY: Luminescent dose response cell-based high throughput screening... -
ATP-dependent molecular chaperone HSP82 EC50 = 750.0 nM 6.12 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Secondary Assay to Identify Inhibitors... -
Unchecked EC50 = 942.0 nM 6.03 PubChem BioAssay. Leishmania major promastigote EC50 determinations. (Class of... -
Unchecked EC50 = 1464.0 nM 5.83 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Retest of Candida albicans Growth in t... -
Unchecked EC50 = 1617.0 nM 5.79 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Compounds that Suppress the... -
Unchecked EC50 = 1895.0 nM 5.72 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Compounds that Suppress the... -
Protein RecA EC50 = 4370.0 nM 5.36 PUBCHEM_BIOASSAY: Fluorescence Cell-Free Homogeneous Dose Retest to Identify Inh... -
Tyrosine-protein kinase JAK2 IC50 = 5197.0 nM 5.28 PUBCHEM_BIOASSAY: Luminescent counterscreen for inhibitors of the Janus kinase 2... -
Peroxisome proliferator-activated receptor gamma/Nuclear receptor coactivator 2 EC50 = 14390.0 nM 4.84 PUBCHEM_BIOASSAY: TR-FRET dose response biochemical High Throughput Screening as... -
Peroxisome proliferator-activated receptor gamma/Nuclear receptor coactivator 1 EC50 = 14900.0 nM 4.83 PUBCHEM_BIOASSAY: TR-FRET dose response biochemical High Throughput Screening as... -
Mannose-6-phosphate isomerase IC50 = 48238.0 nM 4.32 PUBCHEM_BIOASSAY: HTS identification of compounds inhibiting phosphomannose isom... -

Data from ChEMBL 36 via Core Engine