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Compound Detail

CHEMBL1416184

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O=[N+]([O-])c1c(NCCO)cc(Sc2nc3ccccc3s2)c2nonc12

Basic Information

ChEMBL ID CHEMBL1416184
Phase Preclinical
Structure Type MOL
InChI Key PPYQSLDCNMIKJX-UHFFFAOYSA-N
11
Targets
12
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

389.4
MW (Da)
3.30
ALogP
10
HBA
2
HBD
127.2
PSA (Ų)
0.38
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H11N5O4S2
MW 389.42
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -1.92

Activity Summary

EC50 6 meas. best 6.14
IC50 6 meas. best 5.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein RecA
CHEMBL1741171
EC50 6.14 6.14 722.0 1
Type-1 angiotensin II receptor
CHEMBL227
IC50 5.72 5.72 1898.0 1
CHO
CHEMBL613853
IC50 5.71 5.71 1941.0 1
Streptococcus sp. 'group A'
CHEMBL612389
EC50 5.56 5.56 2730.0 1
Streptokinase A
CHEMBL1293228
EC50 5.53 5.53 2946.0 1
Streptococcus
CHEMBL612313
EC50 5.47 5.47 3390.0 1
Toll-like receptor 9
CHEMBL5804
IC50 5.37 5.37 4264.0 1
Beta Lactamase
CHEMBL1293246
IC50 5.04 5.04 9167.0 1
Glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase
CHEMBL1741212
IC50 4.99 4.99 10200.0 1
Unchecked
CHEMBL612545
EC50 4.97 4.96 10716.0 2
Induced myeloid leukemia cell differentiation protein Mcl-1
CHEMBL4361
IC50 4.96 4.96 11050.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein RecA EC50 = 722.0 nM 6.14 PUBCHEM_BIOASSAY: Fluorescence Cell-Free Homogeneous Dose Retest to Identify Inh... -
Type-1 angiotensin II receptor IC50 = 1898.0 nM 5.72 PUBCHEM_BIOASSAY: Dose Response screen for antagonists of Angiotensin II Recepto... -
CHO IC50 = 1941.0 nM 5.71 PUBCHEM_BIOASSAY: Counterscreen for inhibitors of TLR9-MyD88 binding: Luminescen... -
Streptococcus sp. 'group A' EC50 = 2730.0 nM 5.56 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptokinase A EC50 = 2946.0 nM 5.53 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptococcus EC50 = 3390.0 nM 5.47 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... -
Toll-like receptor 9 IC50 = 4264.0 nM 5.37 PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response as... -
Beta Lactamase IC50 = 9167.0 nM 5.04 PUBCHEM_BIOASSAY: Counterscreen for inhibitors of TLR9-MyD88 binding: fluorescen... -
Glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase IC50 = 10200.0 nM 4.99 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS small molecule inhibitors o... -
Unchecked EC50 = 10716.0 nM 4.97 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Compounds that Suppress the... -
Induced myeloid leukemia cell differentiation protein Mcl-1 IC50 = 11050.09 nM 4.96 PUBCHEM_BIOASSAY: Dose Response Confirmation for Mcl-1/Noxa Interaction Inhibito... -
Unchecked EC50 = 11133.0 nM 4.95 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Compounds that Suppress the... -

Data from ChEMBL 36 via Core Engine