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Compound Detail

CHEMBL1407961

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CCC1CCCCN1S(=O)(=O)c1ccc(NC(=O)c2nc(S(C)(=O)=O)ncc2Cl)cc1

Basic Information

ChEMBL ID CHEMBL1407961
Phase Preclinical
Structure Type MOL
InChI Key ISAAEPNCJSJWPZ-UHFFFAOYSA-N
10
Targets
15
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

487.0
MW (Da)
2.74
ALogP
7
HBA
1
HBD
126.4
PSA (Ų)
0.62
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 C19H23ClN4O5S2
MW 487.00
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -2.12

Activity Summary

EC50 9 meas. best 6.18
IC50 6 meas. best 5.93

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Streptokinase A
CHEMBL1293228
EC50 6.18 5.7133 660.0 3
Protein RecA
CHEMBL1741171
EC50 5.96 5.96 1110.0 1
Melanocortin receptor 4
CHEMBL259
IC50 5.93 5.93 1172.0 1
CHO
CHEMBL613853
IC50 5.72 5.72 1910.0 1
G-protein coupled receptor 35
CHEMBL1293267
IC50 5.49 5.49 3233.0 1
Type-1 angiotensin II receptor
CHEMBL227
IC50 5.23 5.23 5897.0 1
Toll-like receptor 9
CHEMBL5804
IC50 5.08 5.08 8336.0 1
Unchecked
CHEMBL612545
EC50 5.01 4.9633 9685.0 3
Beta Lactamase
CHEMBL1293246
IC50 4.96 4.96 11063.0 1
Streptococcus
CHEMBL612313
EC50 4.88 4.83 13239.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Streptokinase A EC50 = 660.0 nM 6.18 PUBCHEM_BIOASSAY: Absorbance Microorganism-Based Dose Response HTS to Identify I... -
Protein RecA EC50 = 1110.0 nM 5.96 PUBCHEM_BIOASSAY: Fluorescence Cell-Free Homogeneous Dose Retest to Identify Inh... -
Streptokinase A EC50 = 1165.0 nM 5.93 PUBCHEM_BIOASSAY: Absorbance Microorganism-Based Dose Response Follow up to Iden... -
Melanocortin receptor 4 IC50 = 1172.0 nM 5.93 PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay fo... -
CHO IC50 = 1910.0 nM 5.72 PUBCHEM_BIOASSAY: Counterscreen for inhibitors of TLR9-MyD88 binding: Luminescen... -
G-protein coupled receptor 35 IC50 = 3233.0 nM 5.49 PUBCHEM_BIOASSAY: Image-Based HTS for Selective Antagonists of GPR35. High conte... -
Type-1 angiotensin II receptor IC50 = 5897.0 nM 5.23 PUBCHEM_BIOASSAY: Dose Response screen for antagonists of Angiotensin II Recepto... -
Toll-like receptor 9 IC50 = 8336.0 nM 5.08 PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response as... -
Streptokinase A EC50 = 9415.0 nM 5.03 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Unchecked EC50 = 9685.0 nM 5.01 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhi... -
Beta Lactamase IC50 = 11063.0 nM 4.96 PUBCHEM_BIOASSAY: Counterscreen for inhibitors of TLR9-MyD88 binding: fluorescen... -
Unchecked EC50 = 11156.0 nM 4.95 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
Unchecked EC50 = 11799.0 nM 4.93 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
Streptococcus EC50 = 13239.0 nM 4.88 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... -
Streptococcus EC50 = 16514.0 nM 4.78 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response Follow up to Id... -

Data from ChEMBL 36 via Core Engine