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Compound Detail

CHEMBL1429929

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CCOC(=O)CCS(=O)(=O)c1nc(-c2ccccc2)cc(C(F)(F)F)n1

Basic Information

ChEMBL ID CHEMBL1429929
Phase Preclinical
Structure Type MOL
InChI Key KAGZAFKDOSGALN-UHFFFAOYSA-N
13
Targets
17
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

388.4
MW (Da)
2.89
ALogP
6
HBA
0
HBD
86.2
PSA (Ų)
0.56
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 C16H15F3N2O4S
MW 388.37
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.32

Activity Summary

IC50 9 meas. best 6.8
EC50 8 meas. best 6.03

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA damage-inducible transcript 3 protein
CHEMBL2146304
IC50 6.8 6.8 160.0 1
Sphingosine 1-phosphate receptor 4
CHEMBL3230
IC50 6.07 5.76 843.0 2
General amino acid permease AGP1
CHEMBL1741178
EC50 6.03 6.03 941.0 1
Protein RecA
CHEMBL1741171
EC50 5.49 5.49 3230.0 1
CHO
CHEMBL613853
IC50 5.46 5.46 3492.0 1
Unchecked
CHEMBL612545
EC50 5.36 4.97 4400.0 4
Signal transducer and activator of transcription 1-alpha/beta
CHEMBL6101
IC50 4.99 4.99 10160.0 1
Toll-like receptor 9
CHEMBL5804
IC50 4.96 4.96 11046.0 1
HT-1080
CHEMBL614580
EC50 4.85 4.85 14000.0 1
Sphingosine 1-phosphate receptor 1
CHEMBL4333
IC50 4.81 4.81 15540.0 1
Nucleic Acid
CHEMBL345
EC50 4.8 4.8 15700.0 1
Signal transducer and activator of transcription 3
CHEMBL4026
IC50 4.62 4.62 24180.0 1
Beta Lactamase
CHEMBL1293246
IC50 4.55 4.55 28223.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA damage-inducible transcript 3 protein IC50 = 160.0 nM 6.8 PUBCHEM_BIOASSAY: CHOP dose-response primary assay. (Class of assay: confirmator... -
Sphingosine 1-phosphate receptor 4 IC50 = 843.0 nM 6.07 PUBCHEM_BIOASSAY: Fluorescence dose response cell-based high throughput screenin... -
General amino acid permease AGP1 EC50 = 941.0 nM 6.03 PUBCHEM_BIOASSAY: Dose Response of TOR pathway GFP-fusion proteins in Saccharomy... -
Protein RecA EC50 = 3230.0 nM 5.49 PUBCHEM_BIOASSAY: Fluorescence Cell-Free Homogeneous Dose Retest to Identify Inh... -
CHO IC50 = 3492.0 nM 5.46 PUBCHEM_BIOASSAY: Counterscreen for inhibitors of TLR9-MyD88 binding: Luminescen... -
Sphingosine 1-phosphate receptor 4 IC50 = 3584.0 nM 5.45 PUBCHEM_BIOASSAY: Late stage fluorescence dose response cell-based screening ass... -
Unchecked EC50 = 4400.0 nM 5.36 PUBCHEM_BIOASSAY: Fluorescent HTS Cytotoxicity/Cell viability assay (HPDE-C7K ce... -
Unchecked EC50 = 4940.0 nM 5.31 PUBCHEM_BIOASSAY: Fluorescent HTS Cytotoxicity/Cell viability assay (HPDE-C7 cel... -
Signal transducer and activator of transcription 1-alpha/beta IC50 = 10160.0 nM 4.99 PUBCHEM_BIOASSAY: Dose response cell-based assay to measure STAT1 inhibition. (C... -
Toll-like receptor 9 IC50 = 11046.0 nM 4.96 PUBCHEM_BIOASSAY: Fluorescence-based cell-based high throughput dose response as... -
HT-1080 EC50 = 14000.0 nM 4.85 PUBCHEM_BIOASSAY: Fluorescent HTS Cytotoxicity/Cell viability assay (HT1080 cell... -
Unchecked EC50 = 14120.0 nM 4.85 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhi... -
Sphingosine 1-phosphate receptor 1 IC50 = 15540.0 nM 4.81 PUBCHEM_BIOASSAY: Fluorescence-based counterscreen assay for S1P4 antagonists: C... -
Nucleic Acid EC50 = 15700.0 nM 4.8 PUBCHEM_BIOASSAY: Luminescent HTS for small molecule inhibitors of MT1-MMP trans... -
Signal transducer and activator of transcription 3 IC50 = 24180.0 nM 4.62 PUBCHEM_BIOASSAY: Dose response counterscreen for STAT1 inhibitors: cell-based h... -
Beta Lactamase IC50 = 28223.0 nM 4.55 PUBCHEM_BIOASSAY: Counterscreen for inhibitors of TLR9-MyD88 binding: fluorescen... -
Unchecked EC50 = 43398.0 nM 4.36 PUBCHEM_BIOASSAY: Luminescent Cell-Based Dose Titration Retest Counterscreen to ... -

Data from ChEMBL 36 via Core Engine