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Compound Detail

CHEMBL1349063

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O=S(=O)(c1ccc2c(c1)C(=NO)c1cc(S(=O)(=O)N3CCCCC3)ccc1-2)N1CCCCC1

Basic Information

ChEMBL ID CHEMBL1349063
Phase Preclinical
Structure Type MOL
InChI Key XYZXEEIUKQGUHB-UHFFFAOYSA-N
3
Targets
14
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

489.6
MW (Da)
3.24
ALogP
6
HBA
1
HBD
107.3
PSA (Ų)
0.45
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 C23H27N3O5S2
MW 489.62
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.87

Activity Summary

EC50 13 meas. best 6.52
IC50 1 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 6.52 5.885 300.0 8
Heat shock factor protein 1
CHEMBL5313
EC50 6.13 6.13 749.0 1
Unchecked
CHEMBL612545
IC50 6.0 6.0 990.0 1
BJ
CHEMBL614358
EC50 5.99 5.6675 1024.0 4

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 300.0 nM 6.52 PUBCHEM_BIOASSAY: Fluorescent HTS Cytotoxicity/Cell viability assay (HPDE-C7 cel... -
Unchecked EC50 = 352.0 nM 6.45 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Compounds that Suppress the... -
Unchecked EC50 = 390.0 nM 6.41 PUBCHEM_BIOASSAY: Fluorescent HTS Cytotoxicity/Cell viability assay (HPDE-C7K ce... -
Unchecked EC50 = 412.0 nM 6.38 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Compounds that Suppress the... -
Heat shock factor protein 1 EC50 = 749.0 nM 6.13 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhi... -
Unchecked IC50 = 990.0 nM 6.0 Inhibition of Wnt/beta-catenin transcriptional activity in human HT-29 cells ass... 26182238
BJ EC50 = 1024.0 nM 5.99 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
BJ EC50 = 2652.0 nM 5.58 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
Unchecked EC50 = 2676.0 nM 5.57 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compound... -
BJ EC50 = 2710.0 nM 5.57 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Comp... -
BJ EC50 = 2970.0 nM 5.53 PUBCHEM_BIOASSAY: Fluorescence Cell-Based Dose Response to Characterize Compound... -
Unchecked EC50 = 3799.0 nM 5.42 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhi... -
Unchecked EC50 = 6009.0 nM 5.22 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
Unchecked EC50 = 7785.0 nM 5.11 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -

Literature References

PubMed DOI Target Context # Activities
26182238 10.1021/acs.jmedchem.5b00460 Unchecked 1
36332549 10.1016/j.ejmech.2022.114861 Unchecked 1

Data from ChEMBL 36 via Core Engine