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Compound Detail

CHEMBL1338317

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O=c1c2ccccc2sn1-c1cc(S(=O)(=O)N2CCOCC2)ccc1N1CCCC1

Basic Information

ChEMBL ID CHEMBL1338317
Phase Preclinical
Structure Type MOL
InChI Key NQBINQNEBDVFFF-UHFFFAOYSA-N
7
Targets
12
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

445.6
MW (Da)
2.67
ALogP
7
HBA
0
HBD
71.8
PSA (Ų)
0.62
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 C21H23N3O4S2
MW 445.57
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.68

Activity Summary

IC50 12 meas. best 5.97

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase
CHEMBL1741212
IC50 5.97 5.23 1080.0 3
Mannose-6-phosphate isomerase
CHEMBL2758
IC50 5.12 5.12 7500.0 2
Phosphoethanolamine/phosphocholine phosphatase
CHEMBL6113
IC50 5.12 5.045 7500.0 2
Carboxy-terminal domain RNA polymerase II polypeptide A small phosphatase 1
CHEMBL1795098
IC50 4.96 4.96 11016.0 1
Unchecked
CHEMBL612545
IC50 4.9 4.9 12490.0 1
Glucose-6-phosphate 1-dehydrogenase
CHEMBL5347
IC50 4.84 4.84 14300.0 1
Phosphomannomutase 2
CHEMBL1741162
IC50 4.53 4.525 29800.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase IC50 = 1080.0 nM 5.97 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS small molecule inhibitors o... -
Mannose-6-phosphate isomerase IC50 = 7510.0 nM 5.12 PUBCHEM_BIOASSAY: Confirmation of compounds inhibiting phosphomannose isomerase ... -
Phosphoethanolamine/phosphocholine phosphatase IC50 = 7500.0 nM 5.12 Inhibition of PHOSPHO1 phosphoethanolamine activity (unknown origin) assessed as... 25124115
Mannose-6-phosphate isomerase IC50 = 7500.0 nM 5.12 Inhibition of phosphomannose isomerase (unknown origin) 25124115
Phosphoethanolamine/phosphocholine phosphatase IC50 = 10700.0 nM 4.97 PUBCHEM_BIOASSAY: SAR assay for compounds that inhibit PHOSPHO1. (Class of assay... -
Carboxy-terminal domain RNA polymerase II polypeptide A small phosphatase 1 IC50 = 11016.0 nM 4.96 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS hits for Scp-1 phosphatase ... -
Unchecked IC50 = 12490.0 nM 4.9 PUBCHEM_BIOASSAY: A biochemical assay using the ADP-Hunter methodology, purified... -
Glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase IC50 = 12500.0 nM 4.9 PUBCHEM_BIOASSAY: Dose Response orthogonal kinetic assay utilizing the direct de... -
Glucose-6-phosphate 1-dehydrogenase IC50 = 14300.0 nM 4.84 PUBCHEM_BIOASSAY: Human Glucose-6-Phosphate Dehydrogenase Dose Response Selectiv... -
Glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase IC50 = 15100.0 nM 4.82 PUBCHEM_BIOASSAY: Dose Response orthogonal assay utilizing the direct end-point ... -
Phosphomannomutase 2 IC50 = 29800.0 nM 4.53 PUBCHEM_BIOASSAY: Counter screen SAR assay for PMM2 inhibitors via a fluorescenc... -
Phosphomannomutase 2 IC50 = 30000.0 nM 4.52 Inhibition of PMM2 (unknown origin) 25124115

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4888484 Plasmodium falciparum 2
25124115 10.1016/j.bmcl.2014.07.013 Phosphoethanolamine/phosphocholine phosphatase 1
25124115 10.1016/j.bmcl.2014.07.013 Mannose-6-phosphate isomerase 1
25124115 10.1016/j.bmcl.2014.07.013 Phosphomannomutase 2 1

Data from ChEMBL 36 via Core Engine