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Compound Detail

CHEMBL1928491

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Oc1ccc(/C=N/Nc2nccnc2Cl)c(O)c1

Basic Information

ChEMBL ID CHEMBL1928491
Phase Preclinical
Structure Type MOL
InChI Key ZZGUTSFAPDWRMW-GIDUJCDVSA-N
4
Targets
21
Activities
3
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

264.7
MW (Da)
1.99
ALogP
6
HBA
3
HBD
90.6
PSA (Ų)
0.58
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 C11H9ClN4O2
MW 264.67
Aromatic Rings 2
Heavy Atoms 18
NP-Likeness -0.85

Activity Summary

EC50 12 meas. best 6.59
IC50 8 meas. best 4.99
Kd 1 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Kd 9.52 9.52 0.3 1
Unchecked
CHEMBL612545
EC50 6.59 5.5557 254.0 7
Luciferin 4-monooxygenase
CHEMBL5567
EC50 5.98 5.98 1047.0 1
BJ
CHEMBL614358
EC50 5.29 5.1075 5074.0 4
NIH3T3
CHEMBL614822
IC50 4.99 4.99 10300.0 1
Unchecked
CHEMBL612545
IC50 4.93 4.3757 11750.0 7

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Kd = 0.3 nM 9.52 Inhibition of Staphylococcus aureus recombinant GST-tagged KAS3 expressed in Esc... 22104972
Unchecked EC50 = 254.0 nM 6.59 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhi... -
Luciferin 4-monooxygenase EC50 = 1047.0 nM 5.98 PUBCHEM_BIOASSAY: Luminescence Biochemical Dose Response HTS to Identify Inhibit... -
Unchecked EC50 = 1390.0 nM 5.86 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Unchecked EC50 = 1630.0 nM 5.79 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Unchecked EC50 = 3698.0 nM 5.43 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhi... -
BJ EC50 = 5074.0 nM 5.29 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Comp... -
BJ EC50 = 6120.0 nM 5.21 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Dose Response to Characterize Compound... -
Unchecked EC50 = 6332.0 nM 5.2 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
Unchecked EC50 = 7095.0 nM 5.15 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
NIH3T3 IC50 = 10300.0 nM 4.99 Cytotoxicity against mouse NIH/3T3 cells after 24 hrs by MTT assay 22104972
BJ EC50 = 10681.0 nM 4.97 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
BJ EC50 = 10918.0 nM 4.96 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Unchecked IC50 = 11750.0 nM 4.93 PUBCHEM_BIOASSAY: A biochemical assay using the ADP-Hunter methodology, purified... -
Unchecked EC50 = 13364.0 nM 4.87 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Unchecked IC50 = 30490.0 nM 4.52 PUBCHEM_BIOASSAY: A counter screen for small molecule screen for inhibitors of t... -
Unchecked IC50 = 35040.0 nM 4.46 PUBCHEM_BIOASSAY: A Counter Screen to identiry small molecule screen for inhibit... -
Unchecked IC50 = 63200.0 nM 4.2 PUBCHEM_BIOASSAY: A screen for inhibitors of the PhoP region in Salmonella Typhi... -
Unchecked IC50 = 64810.0 nM 4.19 PUBCHEM_BIOASSAY: A small molecule screen for inhibitors of the PhoP region in S... -
Unchecked IC50 = 65751.0 nM 4.18 PUBCHEM_BIOASSAY: A screen for inhibitors of the PhoP region in Salmonella Typhi... -

Literature References

PubMed DOI Target Context # Activities
22104972 10.1016/j.ejmech.2011.10.052 Staphylococcus aureus 2
22104972 10.1016/j.ejmech.2011.10.052 NIH3T3 2
22104972 10.1016/j.ejmech.2011.10.052 Escherichia coli 1
22104972 10.1016/j.ejmech.2011.10.052 Enterococcus faecalis 1
22104972 10.1016/j.ejmech.2011.10.052 Enterococcus faecium 1
22104972 10.1016/j.ejmech.2011.10.052 Unchecked 1

Data from ChEMBL 36 via Core Engine