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Compound Detail

CHEMBL1424189

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CCOC(=O)C1=C(C)N=c2sc(=Cc3ccc(OCC(=O)O)cc3)c(=O)n2C1c1ccc(Cl)cc1

Basic Information

ChEMBL ID CHEMBL1424189
Phase Preclinical
Structure Type MOL
InChI Key XSQDEOJNULNBPG-UHFFFAOYSA-N
6
Targets
10
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

513.0
MW (Da)
2.92
ALogP
8
HBA
1
HBD
107.2
PSA (Ų)
0.49
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 C25H21ClN2O6S
MW 512.97
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.45

Activity Summary

IC50 10 meas. best 6.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein phosphatase non-receptor type 7
CHEMBL2219
IC50 6.38 6.33 419.0 2
Dual specificity protein phosphatase 3
CHEMBL2635
IC50 5.68 5.5167 2080.0 3
Tyrosine-protein phosphatase non-receptor type 12
CHEMBL3236
IC50 5.62 5.62 2410.0 1
Tyrosine-protein phosphatase non-receptor type 22
CHEMBL2889
IC50 5.56 5.49 2740.0 2
DNA (cytosine-5)-methyltransferase 1
CHEMBL1993
IC50 5.08 5.08 8420.0 1
Dual specificity protein phosphatase 6
CHEMBL5511
IC50 4.38 4.38 41367.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein phosphatase non-receptor type 7 IC50 = 419.0 nM 6.38 PUBCHEM_BIOASSAY: SAR analysis of compounds that inhibit HePTP - Set 2. (Class o... -
Tyrosine-protein phosphatase non-receptor type 7 IC50 = 520.0 nM 6.28 PUBCHEM_BIOASSAY: MOA HePTP Fluorescent secondary assay for identification of re... -
Dual specificity protein phosphatase 3 IC50 = 2080.0 nM 5.68 PUBCHEM_BIOASSAY: MOA VHR1 Fluorescent secondary assay for identification of red... -
Tyrosine-protein phosphatase non-receptor type 12 IC50 = 2410.0 nM 5.62 PUBCHEM_BIOASSAY: SAR Selectivity Analysis of small molecule inhibitors of PEST ... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 2740.0 nM 5.56 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using pCAP substrate for In Vitro d... -
Dual specificity protein phosphatase 3 IC50 = 3200.0 nM 5.5 PUBCHEM_BIOASSAY: SAR VHR1 Fluorescent Assay for In Vitro dose response studies.... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 3820.0 nM 5.42 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using OMFP substrate for In Vitro d... -
Dual specificity protein phosphatase 3 IC50 = 4230.0 nM 5.37 PUBCHEM_BIOASSAY: SAR VHR1 absorbance Assay for In Vitro dose response studies. ... -
DNA (cytosine-5)-methyltransferase 1 IC50 = 8420.0 nM 5.08 PUBCHEM_BIOASSAY: Dose response confirmation of DNMT1 inhibitors in a Fluorescen... -
Dual specificity protein phosphatase 6 IC50 = 41367.0 nM 4.38 PUBCHEM_BIOASSAY: In Vitro MKP-3 Dose Response Assay for SAR Study. (Class of as... -

Data from ChEMBL 36 via Core Engine