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Compound Detail

CHEMBL1373210

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Cc1ccc(NC(=O)CN2C(=O)S/C(=C\c3cc(Cl)c(OCC(=O)O)c(Cl)c3)C2=O)cc1

Basic Information

ChEMBL ID CHEMBL1373210
Phase Preclinical
Structure Type MOL
InChI Key JXYIXQGHGKYZLG-PXNMLYILSA-N
7
Targets
10
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

495.3
MW (Da)
4.44
ALogP
6
HBA
2
HBD
113.0
PSA (Ų)
0.55
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H16Cl2N2O6S
MW 495.34
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -1.83

Activity Summary

IC50 10 meas. best 6.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein phosphatase non-receptor type 7
CHEMBL2219
IC50 6.22 6.155 596.0 2
Carboxy-terminal domain RNA polymerase II polypeptide A small phosphatase 1
CHEMBL1795098
IC50 5.6 5.6 2503.0 1
Tyrosine-protein phosphatase non-receptor type 12
CHEMBL3236
IC50 5.55 5.55 2790.0 1
Dual specificity protein phosphatase 3
CHEMBL2635
IC50 5.45 5.45 3550.0 1
Tyrosine-protein phosphatase non-receptor type 22
CHEMBL2889
IC50 5.4 5.395 3950.0 2
SUMO-activating enzyme
CHEMBL2095174
IC50 5.09 4.98 8110.0 2
Dual specificity protein phosphatase 6
CHEMBL5511
IC50 4.75 4.75 17800.0 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 = 596.0 nM 6.22 PUBCHEM_BIOASSAY: SAR analysis of compounds that inhibit HePTP - Set 2. (Class o... -
Tyrosine-protein phosphatase non-receptor type 7 IC50 = 819.0 nM 6.09 PUBCHEM_BIOASSAY: MOA HePTP Fluorescent secondary assay for identification of re... -
Carboxy-terminal domain RNA polymerase II polypeptide A small phosphatase 1 IC50 = 2503.0 nM 5.6 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS hits for Scp-1 phosphatase ... -
Tyrosine-protein phosphatase non-receptor type 12 IC50 = 2790.0 nM 5.55 PUBCHEM_BIOASSAY: SAR Selectivity Analysis of small molecule inhibitors of PEST ... -
Dual specificity protein phosphatase 3 IC50 = 3550.0 nM 5.45 PUBCHEM_BIOASSAY: SAR VHR1 Fluorescent Assay for In Vitro dose response studies ... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 3950.0 nM 5.4 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using OMFP substrate for In Vitro d... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 4090.0 nM 5.39 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using pCAP substrate for In Vitro d... -
SUMO-activating enzyme IC50 = 8110.0 nM 5.09 PUBCHEM_BIOASSAY: AlphaScreen confirmatory assay for validation of inhibitors of... -
SUMO-activating enzyme IC50 = 13550.0 nM 4.87 PUBCHEM_BIOASSAY: uHTS HTRF assay for identification of inhibitors of SUMOylatio... -
Dual specificity protein phosphatase 6 IC50 = 17800.0 nM 4.75 PUBCHEM_BIOASSAY: In Vitro MKP-3 Dose Response Assay for SAR Study. (Class of as... -

Data from ChEMBL 36 via Core Engine