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Compound Detail

CHEMBL1315948

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CCc1ccc(Nc2n[n+](-c3ccccc3)c(-c3c(Cl)cccc3Cl)s2)cc1.[Cl-]

Basic Information

ChEMBL ID CHEMBL1315948
Phase Preclinical
Structure Type MOL
InChI Key BQOXWTWXGDCHGV-UHFFFAOYSA-M
Parent Compound CHEMBL1617450
Active Moiety CHEMBL1617450
10
Targets
14
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

427.4
MW (Da)
6.70
ALogP
3
HBA
1
HBD
28.8
PSA (Ų)
0.36
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H18Cl3N3S
MW 462.83
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -1.06

Activity Summary

EC50 10 meas. best 5.87
IC50 4 meas. best 5.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 5.87 5.52 1355.0 3
Beta Lactamase
CHEMBL1293246
IC50 5.5 5.5 3124.0 1
Streptococcus sp. 'group A'
CHEMBL612389
EC50 5.45 5.45 3578.0 1
Toll-like receptor 9
CHEMBL5804
IC50 5.34 5.34 4596.0 1
Streptokinase A
CHEMBL1293228
EC50 5.21 5.17 6220.0 2
CHO
CHEMBL613853
IC50 5.17 5.17 6785.0 1
Opioid receptors; mu & delta
CHEMBL2095149
EC50 5.04 5.04 9079.0 1
Protein RecA
CHEMBL1741171
EC50 5.03 5.03 9380.0 1
Streptococcus
CHEMBL612313
EC50 4.99 4.99 10350.0 1
Delta-type opioid receptor
CHEMBL236
EC50 4.85 4.85 14159.0 1
Unchecked
CHEMBL612545
IC50 4.38 4.38 41290.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 1355.0 nM 5.87 PUBCHEM_BIOASSAY: Luminescence Cell-Based/Microorganism Dose Confirmation HTS to... -
Beta Lactamase IC50 = 3124.0 nM 5.5 PUBCHEM_BIOASSAY: Counterscreen for inhibitors of TLR9-MyD88 binding: fluorescen... -
Streptococcus sp. 'group A' EC50 = 3578.0 nM 5.45 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Unchecked EC50 = 3750.0 nM 5.43 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Toll-like receptor 9 IC50 = 4596.0 nM 5.34 PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response as... -
Unchecked EC50 = 5531.0 nM 5.26 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS Screen to Identify C... -
Streptokinase A EC50 = 6220.0 nM 5.21 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
CHO IC50 = 6785.0 nM 5.17 PUBCHEM_BIOASSAY: Counterscreen for inhibitors of TLR9-MyD88 binding: Luminescen... -
Streptokinase A EC50 = 7404.0 nM 5.13 PUBCHEM_BIOASSAY: Absorbance Microorganism-Based Dose Response HTS to Identify I... -
Opioid receptors; mu & delta EC50 = 9079.0 nM 5.04 PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response as... -
Protein RecA EC50 = 9380.0 nM 5.03 PUBCHEM_BIOASSAY: Fluorescence Cell-Free Homogeneous Dose Retest to Identify Inh... -
Streptococcus EC50 = 10350.0 nM 4.99 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... -
Delta-type opioid receptor EC50 = 14159.0 nM 4.85 PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (... -
Unchecked IC50 = 41290.0 nM 4.38 PUBCHEM_BIOASSAY: A counter screen for small molecule screen for inhibitors of t... -

Data from ChEMBL 36 via Core Engine