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Compound Detail

CHEMBL546170

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COc1cccc2sc(Nc3nc(-c4ccccn4)cs3)nc12

Basic Information

ChEMBL ID CHEMBL546170
Phase Preclinical
Structure Type MOL
InChI Key WSJSWLQVPVZOKR-UHFFFAOYSA-N
8
Targets
17
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

340.4
MW (Da)
4.57
ALogP
7
HBA
1
HBD
59.9
PSA (Ų)
0.59
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 C16H12N4OS2
MW 340.43
Aromatic Rings 4
Heavy Atoms 23
NP-Likeness -2.15

Activity Summary

EC50 11 meas. best 6.9
IC50 6 meas. best 5.86

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 6.9 5.2171 126.0 7
Unchecked
CHEMBL612545
IC50 5.86 5.86 1396.0 1
Kappa-type opioid receptor
CHEMBL237
IC50 5.79 5.79 1620.0 1
Large ribosomal subunit protein eL19A
CHEMBL1741172
EC50 5.42 5.42 3822.0 1
Sentrin-specific protease 7
CHEMBL1741213
IC50 5.36 5.36 4380.0 1
Sentrin-specific protease 6
CHEMBL1741215
IC50 5.22 5.22 6040.0 1
BJ
CHEMBL614358
EC50 5.1 4.9767 8015.0 3
Mitochondrial import inner membrane translocase subunit TIM10
CHEMBL1741194
IC50 4.7 4.7 20200.0 1
Caspase-3
CHEMBL2334
IC50 4.5 4.5 31700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 126.0 nM 6.9 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
Unchecked IC50 = 1396.0 nM 5.86 PUBCHEM_BIOASSAY: Luminescence-based dose response cell-based high throughput sc... -
Kappa-type opioid receptor IC50 = 1620.0 nM 5.79 PUBCHEM_BIOASSAY: uHTS identification of small molecule antagonists of the kappa... -
Unchecked EC50 = 1650.0 nM 5.78 PUBCHEM_BIOASSAY: Dose response confirmation of small molecule activators of the... -
Unchecked EC50 = 2228.0 nM 5.65 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhi... -
Large ribosomal subunit protein eL19A EC50 = 3822.0 nM 5.42 PUBCHEM_BIOASSAY: Dose Response of TOR pathway GFP-fusion proteins in Saccharomy... -
Sentrin-specific protease 7 IC50 = 4380.0 nM 5.36 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
Sentrin-specific protease 6 IC50 = 6040.0 nM 5.22 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
Unchecked EC50 = 6910.0 nM 5.16 PUBCHEM_BIOASSAY: Luminescent Cell-Based Dose Titration Retest Counterscreen to ... -
BJ EC50 = 8015.0 nM 5.1 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
BJ EC50 = 12153.0 nM 4.92 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Comp... -
BJ EC50 = 12333.0 nM 4.91 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Unchecked EC50 = 17521.0 nM 4.76 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Mitochondrial import inner membrane translocase subunit TIM10 IC50 = 20200.0 nM 4.7 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS small molecule inhibitors o... -
Caspase-3 IC50 = 31700.0 nM 4.5 PUBCHEM_BIOASSAY: Dose Response confirmation of inhibitors of Sentrin-specific p... -
Unchecked EC50 = 64506.0 nM 4.19 PUBCHEM_BIOASSAY: Luminescence Cell-Based Confirmation at Dose to Identify Trans... -
Unchecked EC50 = 84119.0 nM 4.08 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -

Literature References

PubMed DOI Target Context # Activities
20485427 10.1038/nature09107 Plasmodium falciparum 4
20485427 10.1038/nature09107 HepG2 1
20485427 10.1038/nature09107 Unchecked 1
- 10.6019/CHEMBL3433997 Glucose transporter 1
- 10.6019/CHEMBL3433997 Solute carrier family 2, facilitated glucose transporter member 1 1
- 10.6019/CHEMBL3433997 Hexose transporter 1 1

Data from ChEMBL 36 via Core Engine