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Compound Detail

CHEMBL1445488

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CCOC(=O)c1sc2nc3c(SCC(=O)O)cc(C(=O)c4ccccc4O)cn3c(=O)c2c1C

Basic Information

ChEMBL ID CHEMBL1445488
Phase Preclinical
Structure Type MOL
InChI Key WRFNFMUNJVHPGT-UHFFFAOYSA-N
10
Targets
16
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

498.5
MW (Da)
3.51
ALogP
10
HBA
2
HBD
135.3
PSA (Ų)
0.22
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 C23H18N2O7S2
MW 498.54
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.30

Activity Summary

IC50 16 meas. best 6.98

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein phosphatase non-receptor type 7
CHEMBL2219
IC50 6.98 6.98 105.0 1
Dual specificity protein phosphatase 3
CHEMBL2635
IC50 6.66 6.0017 218.0 6
72 kDa type IV collagenase
CHEMBL333
IC50 6.09 6.09 821.0 1
Tyrosine-protein phosphatase non-receptor type 11
CHEMBL3864
IC50 5.97 5.97 1080.0 1
Tyrosine-protein phosphatase non-receptor type 5
CHEMBL2007628
IC50 5.66 5.66 2180.0 1
DNA (cytosine-5)-methyltransferase 1
CHEMBL1993
IC50 5.38 5.38 4120.0 1
26S proteasome non-ATPase regulatory subunit 14
CHEMBL2007629
IC50 5.17 5.17 6790.0 1
Carboxy-terminal domain RNA polymerase II polypeptide A small phosphatase 1
CHEMBL1795098
IC50 4.83 4.83 14782.0 1
Prothrombin
CHEMBL4471
IC50 4.25 4.25 56600.0 1
Dual specificity protein phosphatase 6
CHEMBL5511
IC50 4.24 4.24 57300.0 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 = 105.0 nM 6.98 PUBCHEM_BIOASSAY: MOA HePTP Fluorescent secondary assay for identification of re... -
Dual specificity protein phosphatase 3 IC50 = 218.0 nM 6.66 PUBCHEM_BIOASSAY: SAR VHR1 Fluorescent Assay for In Vitro dose response studies ... -
Dual specificity protein phosphatase 3 IC50 = 382.0 nM 6.42 PUBCHEM_BIOASSAY: SAR VHR1 Fluorescent Assay for In Vitro dose response studies.... -
Dual specificity protein phosphatase 3 IC50 = 549.0 nM 6.26 PUBCHEM_BIOASSAY: Dose Response selectivity of inhibitors of STriatal-Enriched P... -
72 kDa type IV collagenase IC50 = 821.0 nM 6.09 PUBCHEM_BIOASSAY: Dose Response validation of uHTS RPN11 inhibitor hits using a ... -
Tyrosine-protein phosphatase non-receptor type 11 IC50 = 1080.0 nM 5.97 PUBCHEM_BIOASSAY: Dose Response selectivity of inhibitors of Striatal-Enriched P... -
Dual specificity protein phosphatase 3 IC50 = 1240.0 nM 5.91 PUBCHEM_BIOASSAY: SAR VHR1 absorbance Assay for In Vitro dose response studies. ... -
Tyrosine-protein phosphatase non-receptor type 5 IC50 = 2180.0 nM 5.66 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS small molecule inhibitors o... -
Dual specificity protein phosphatase 3 IC50 = 3690.0 nM 5.43 PUBCHEM_BIOASSAY: Fluorescent assay for identification of compounds that inhibit... -
DNA (cytosine-5)-methyltransferase 1 IC50 = 4120.0 nM 5.38 PUBCHEM_BIOASSAY: Dose response confirmation of DNMT1 inhibitors in a Fluorescen... -
Dual specificity protein phosphatase 3 IC50 = 4640.0 nM 5.33 PUBCHEM_BIOASSAY: uHTS absorbance assay for the identification of compounds that... -
26S proteasome non-ATPase regulatory subunit 14 IC50 = 6790.0 nM 5.17 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS RPN11 inhibitor hits in a F... -
Carboxy-terminal domain RNA polymerase II polypeptide A small phosphatase 1 IC50 = 14782.0 nM 4.83 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS hits for Scp-1 phosphatase ... -
Prothrombin IC50 = 56600.0 nM 4.25 PUBCHEM_BIOASSAY: Dose Response validation of uHTS RPN11 inhibitor hits using a ... -
Dual specificity protein phosphatase 6 IC50 = 57300.0 nM 4.24 PUBCHEM_BIOASSAY: In Vitro MKP-3 Dose Response Assay for SAR Study. (Class of as... -

Data from ChEMBL 36 via Core Engine