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Compound Detail

CHEMBL1438889

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COc1ccc(/C=C2\SC(=S)N(CCC(=O)Nc3ccc(C(=O)O)cc3)C2=O)cc1OC

Basic Information

ChEMBL ID CHEMBL1438889
Phase Preclinical
Structure Type MOL
InChI Key SXQHJEJEQMJASD-PDGQHHTCSA-N
6
Targets
17
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

472.5
MW (Da)
3.63
ALogP
7
HBA
2
HBD
105.2
PSA (Ų)
0.44
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H20N2O6S2
MW 472.54
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -1.50

Activity Summary

IC50 15 meas. best 6.51
EC50 2 meas. best 5.03

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein phosphatase non-receptor type 7
CHEMBL2219
IC50 6.51 5.7267 312.0 3
Tyrosine-protein phosphatase non-receptor type 22
CHEMBL2889
IC50 5.97 5.51 1080.0 10
Tyrosine-protein phosphatase non-receptor type 12
CHEMBL3236
IC50 5.95 5.95 1130.0 1
Voltage-gated N-type calcium channel alpha-1B subunit/Amyloid beta A4 precursor protein-binding family A member 1
CHEMBL2097170
IC50 5.1 5.1 7890.0 1
Apoptotic protease-activating factor 1
CHEMBL1795093
EC50 5.03 5.03 9360.0 1
Unchecked
CHEMBL612545
EC50 4.84 4.84 14600.0 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 = 312.0 nM 6.51 PUBCHEM_BIOASSAY: SAR analysis of compounds that inhibit HePTP - Set 2. (Class o... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 1080.0 nM 5.97 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using OMFP substrate for In Vitro d... -
Tyrosine-protein phosphatase non-receptor type 12 IC50 = 1130.0 nM 5.95 PUBCHEM_BIOASSAY: SAR Selectivity Analysis of small molecule inhibitors of PEST ... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 1380.0 nM 5.86 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using pCAP substrate for In Vitro d... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 2755.0 nM 5.56 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS hits from a small molecule ... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 2940.0 nM 5.53 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using pCAP substrate for In Vitro d... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 2957.0 nM 5.53 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using pCAP substrate for In Vitro d... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 3741.0 nM 5.43 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS hits from a small molecule ... -
Tyrosine-protein phosphatase non-receptor type 7 IC50 = 3780.0 nM 5.42 PUBCHEM_BIOASSAY: Dose Response confirmation of HTS hits from an HePTP Fluoresce... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 4090.0 nM 5.39 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using OMFP substrate for In Vitro d... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 4289.14 nM 5.37 PUBCHEM_BIOASSAY: uHTS identification of small molecule inhibitors of LYP via a ... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 4659.16 nM 5.33 PUBCHEM_BIOASSAY: LYP1 Fluorescent Assay using OMFP substrate for In Vitro dose ... -
Tyrosine-protein phosphatase non-receptor type 7 IC50 = 5640.0 nM 5.25 PUBCHEM_BIOASSAY: HTS HePTP Fluorescent Assay using OMFP substrate for In Vitro ... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 7461.0 nM 5.13 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using OMFP substrate for In Vitro d... -
Voltage-gated N-type calcium channel alpha-1B subunit/Amyloid beta A4 precursor protein-binding family A member 1 IC50 = 7890.0 nM 5.1 PUBCHEM_BIOASSAY: Homogeneous Time-Resolved Fluorescence Resonance Energy Transf... -
Apoptotic protease-activating factor 1 EC50 = 9360.0 nM 5.03 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS Activators of the Apaf-1 Pa... -
Unchecked EC50 = 14600.0 nM 4.84 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 activators ... -

Data from ChEMBL 36 via Core Engine