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Compound Detail

CHEMBL1414679

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CC1=C(C(=O)OC(C)C)C(c2ccc(Cl)cc2)n2c(sc(=Cc3ccc(OCC(=O)O)cc3)c2=O)=N1

Basic Information

ChEMBL ID CHEMBL1414679
Phase Preclinical
Structure Type MOL
InChI Key IOSUGCLQHJKTCK-UHFFFAOYSA-N
6
Targets
10
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

527.0
MW (Da)
3.30
ALogP
8
HBA
1
HBD
107.2
PSA (Ų)
0.47
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 C26H23ClN2O6S
MW 527.00
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -1.41

Activity Summary

IC50 10 meas. best 6.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein phosphatase non-receptor type 7
CHEMBL2219
IC50 6.52 6.465 304.0 2
Dual specificity protein phosphatase 3
CHEMBL2635
IC50 6.01 5.5433 967.0 3
Tyrosine-protein phosphatase non-receptor type 12
CHEMBL3236
IC50 5.78 5.78 1680.0 1
Tyrosine-protein phosphatase non-receptor type 22
CHEMBL2889
IC50 5.44 5.42 3630.0 2
DNA (cytosine-5)-methyltransferase 1
CHEMBL1993
IC50 5.26 5.26 5430.0 1
Dual specificity protein phosphatase 6
CHEMBL5511
IC50 4.38 4.38 41833.0 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 = 304.0 nM 6.52 PUBCHEM_BIOASSAY: SAR analysis of compounds that inhibit HePTP - Set 2. (Class o... -
Tyrosine-protein phosphatase non-receptor type 7 IC50 = 391.0 nM 6.41 PUBCHEM_BIOASSAY: MOA HePTP Fluorescent secondary assay for identification of re... -
Dual specificity protein phosphatase 3 IC50 = 967.0 nM 6.01 PUBCHEM_BIOASSAY: SAR VHR1 absorbance Assay for In Vitro dose response studies. ... -
Tyrosine-protein phosphatase non-receptor type 12 IC50 = 1680.0 nM 5.78 PUBCHEM_BIOASSAY: SAR Selectivity Analysis of small molecule inhibitors of PEST ... -
Dual specificity protein phosphatase 3 IC50 = 1930.0 nM 5.71 PUBCHEM_BIOASSAY: MOA VHR1 Fluorescent secondary assay for identification of red... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 3630.0 nM 5.44 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using pCAP substrate for In Vitro d... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 4010.0 nM 5.4 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using OMFP substrate for In Vitro d... -
DNA (cytosine-5)-methyltransferase 1 IC50 = 5430.0 nM 5.26 PUBCHEM_BIOASSAY: Dose response confirmation of DNMT1 inhibitors in a Fluorescen... -
Dual specificity protein phosphatase 3 IC50 = 12300.0 nM 4.91 PUBCHEM_BIOASSAY: SAR VHR1 Fluorescent Assay for In Vitro dose response studies.... -
Dual specificity protein phosphatase 6 IC50 = 41833.0 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