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Compound Detail

CHEMBL1603615

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O=C(Nc1ccccc1)Nc1cc(OCC(F)(F)F)cc(OCC(F)(F)F)c1

Basic Information

ChEMBL ID CHEMBL1603615
Phase Preclinical
Structure Type MOL
InChI Key PXWNITNHJVSBTL-UHFFFAOYSA-N
10
Targets
15
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

408.3
MW (Da)
5.21
ALogP
3
HBA
2
HBD
59.6
PSA (Ų)
0.65
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H14F6N2O3
MW 408.30
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -1.32

Activity Summary

EC50 8 meas. best 6.14
IC50 7 meas. best 7.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sphingosine 1-phosphate receptor 4
CHEMBL3230
IC50 7.08 6.83 82.7 2
Unchecked
CHEMBL612545
EC50 6.14 5.4175 719.0 4
Sphingosine 1-phosphate receptor 5
CHEMBL2274
IC50 5.89 5.89 1299.0 1
Sphingosine 1-phosphate receptor 3
CHEMBL3892
IC50 5.78 5.78 1678.0 1
DNA damage-inducible transcript 3 protein
CHEMBL2146304
IC50 5.63 5.63 2340.0 1
Sphingosine 1-phosphate receptor 2
CHEMBL2955
IC50 5.63 5.63 2349.0 1
X-box-binding protein 1
CHEMBL1741176
IC50 5.4 5.4 3950.0 1
Streptococcus sp. 'group A'
CHEMBL612389
EC50 5.34 5.34 4556.0 1
Streptokinase A
CHEMBL1293228
EC50 5.32 5.03 4782.0 2
Streptococcus
CHEMBL612313
EC50 5.02 5.02 9634.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sphingosine 1-phosphate receptor 4 IC50 = 82.66 nM 7.08 PUBCHEM_BIOASSAY: Late stage fluorescence dose response cell-based screening ass... -
Sphingosine 1-phosphate receptor 4 IC50 = 260.0 nM 6.58 PUBCHEM_BIOASSAY: Fluorescence dose response cell-based high throughput screenin... -
Unchecked EC50 = 719.0 nM 6.14 PUBCHEM_BIOASSAY: Luminescence Cell-Based/Microorganism Dose Confirmation HTS to... -
Sphingosine 1-phosphate receptor 5 IC50 = 1299.0 nM 5.89 PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluoresce... -
Sphingosine 1-phosphate receptor 3 IC50 = 1678.0 nM 5.78 PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluoresce... -
Sphingosine 1-phosphate receptor 2 IC50 = 2349.0 nM 5.63 PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluoresce... -
DNA damage-inducible transcript 3 protein IC50 = 2340.0 nM 5.63 PUBCHEM_BIOASSAY: CHOP dose-response primary assay. (Class of assay: confirmator... -
X-box-binding protein 1 IC50 = 3950.0 nM 5.4 PUBCHEM_BIOASSAY: XBP1 DR counterscreen for CHOP. (Class of assay: confirmatory)... -
Streptococcus sp. 'group A' EC50 = 4556.0 nM 5.34 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptokinase A EC50 = 4782.0 nM 5.32 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Unchecked EC50 = 6086.0 nM 5.22 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhi... -
Unchecked EC50 = 6808.0 nM 5.17 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
Unchecked EC50 = 7181.0 nM 5.14 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
Streptococcus EC50 = 9634.0 nM 5.02 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... -
Streptokinase A EC50 = 18136.0 nM 4.74 PUBCHEM_BIOASSAY: Absorbance Microorganism-Based Dose Response HTS to Identify I... -

Data from ChEMBL 36 via Core Engine