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Compound Detail

CHEMBL1412583

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CCOC(=O)/C(=C\c1ccc(OC(F)F)cc1)C1=Nn2c(nnc2-c2ccc(Cl)cc2)SC1

Basic Information

ChEMBL ID CHEMBL1412583
Phase Preclinical
Structure Type MOL
InChI Key IHJCKBWPCNFLBM-BOPFTXTBSA-N
9
Targets
12
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

490.9
MW (Da)
5.16
ALogP
8
HBA
0
HBD
78.6
PSA (Ų)
0.34
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H17ClF2N4O3S
MW 490.92
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.54

Activity Summary

IC50 8 meas. best 7.47
EC50 4 meas. best 5.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sphingosine 1-phosphate receptor 5
CHEMBL2274
IC50 7.47 7.47 34.0 1
Sphingosine 1-phosphate receptor 4
CHEMBL3230
IC50 6.78 6.625 168.0 2
Sphingosine 1-phosphate receptor 1
CHEMBL4333
IC50 6.46 5.835 351.0 2
Sphingosine 1-phosphate receptor 3
CHEMBL3892
IC50 6.31 6.31 493.9 1
Sphingosine 1-phosphate receptor 2
CHEMBL2955
IC50 6.21 6.21 614.2 1
X-box-binding protein 1
CHEMBL1741176
IC50 5.33 5.33 4700.0 1
Heat shock factor protein 1
CHEMBL5313
EC50 5.18 5.18 6619.0 1
Unchecked
CHEMBL612545
EC50 5.01 5.0 9668.0 2
Integrin alpha-4
CHEMBL278
EC50 4.93 4.93 11820.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sphingosine 1-phosphate receptor 5 IC50 = 34.0 nM 7.47 PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluoresce... -
Sphingosine 1-phosphate receptor 4 IC50 = 168.0 nM 6.78 PUBCHEM_BIOASSAY: Fluorescence dose response cell-based high throughput screenin... -
Sphingosine 1-phosphate receptor 4 IC50 = 342.1 nM 6.47 PUBCHEM_BIOASSAY: Late stage fluorescence dose response cell-based screening ass... -
Sphingosine 1-phosphate receptor 1 IC50 = 351.0 nM 6.46 PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluoresce... -
Sphingosine 1-phosphate receptor 3 IC50 = 493.9 nM 6.31 PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluoresce... -
Sphingosine 1-phosphate receptor 2 IC50 = 614.2 nM 6.21 PUBCHEM_BIOASSAY: Late stage counterscreen assay for S1P4 antagonists: Fluoresce... -
X-box-binding protein 1 IC50 = 4700.0 nM 5.33 PUBCHEM_BIOASSAY: XBP1 DR counterscreen for CHOP. (Class of assay: confirmatory)... -
Sphingosine 1-phosphate receptor 1 IC50 = 6099.0 nM 5.21 PUBCHEM_BIOASSAY: Fluorescence-based counterscreen assay for S1P4 antagonists: C... -
Heat shock factor protein 1 EC50 = 6619.0 nM 5.18 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhi... -
Unchecked EC50 = 9668.0 nM 5.01 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Compounds that Suppress the... -
Unchecked EC50 = 10192.0 nM 4.99 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Compounds that Suppress the... -
Integrin alpha-4 EC50 = 11820.0 nM 4.93 PUBCHEM_BIOASSAY: SAR Confirmatory Dose Response LIBS Assay for Allosteric Ligan... -

Data from ChEMBL 36 via Core Engine