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Compound Detail

CHEMBL1407368

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COc1cc(/C=C2\SC(=O)N(CC(=O)Nc3ccc(C)cc3)C2=O)cc(Cl)c1OCC(=O)O

Basic Information

ChEMBL ID CHEMBL1407368
Phase Preclinical
Structure Type MOL
InChI Key LVKWYVRJCVWPCV-MFOYZWKCSA-N
7
Targets
11
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

490.9
MW (Da)
3.80
ALogP
7
HBA
2
HBD
122.2
PSA (Ų)
0.54
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 C22H19ClN2O7S
MW 490.92
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.76

Activity Summary

IC50 11 meas. best 6.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein phosphatase non-receptor type 7
CHEMBL2219
IC50 6.59 6.59 256.0 1
Tyrosine-protein phosphatase non-receptor type 12
CHEMBL3236
IC50 6.5 6.5 313.0 1
Tyrosine-protein phosphatase non-receptor type 22
CHEMBL2889
IC50 6.09 5.955 803.0 2
Dual specificity protein phosphatase 3
CHEMBL2635
IC50 5.93 5.6167 1180.0 3
Serine/threonine-protein phosphatase PP1-alpha catalytic subunit
CHEMBL2164
IC50 5.21 5.21 6238.0 1
Dual specificity protein phosphatase 6
CHEMBL5511
IC50 5.18 4.65 6660.0 2
Voltage-gated N-type calcium channel alpha-1B subunit/Amyloid beta A4 precursor protein-binding family A member 1
CHEMBL2097170
IC50 5.16 5.16 6910.0 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 = 256.0 nM 6.59 PUBCHEM_BIOASSAY: MOA HePTP Fluorescent secondary assay for identification of re... -
Tyrosine-protein phosphatase non-receptor type 12 IC50 = 313.0 nM 6.5 PUBCHEM_BIOASSAY: SAR Selectivity Analysis of small molecule inhibitors of PEST ... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 803.0 nM 6.09 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using pCAP substrate for In Vitro d... -
Dual specificity protein phosphatase 3 IC50 = 1180.0 nM 5.93 PUBCHEM_BIOASSAY: SAR VHR1 Fluorescent Assay for In Vitro dose response studies.... -
Tyrosine-protein phosphatase non-receptor type 22 IC50 = 1510.0 nM 5.82 PUBCHEM_BIOASSAY: SAR LYP1 Fluorescent Assay using OMFP substrate for In Vitro d... -
Dual specificity protein phosphatase 3 IC50 = 2400.0 nM 5.62 PUBCHEM_BIOASSAY: SAR VHR1 absorbance Assay for In Vitro dose response studies. ... -
Dual specificity protein phosphatase 3 IC50 = 5010.0 nM 5.3 PUBCHEM_BIOASSAY: uHTS absorbance assay for the identification of compounds that... -
Serine/threonine-protein phosphatase PP1-alpha catalytic subunit IC50 = 6238.0 nM 5.21 PUBCHEM_BIOASSAY: Fluorescence-based biochemical high throughput dose response a... -
Dual specificity protein phosphatase 6 IC50 = 6660.0 nM 5.18 PUBCHEM_BIOASSAY: In Vitro MKP-3 Dose Response Assay for SAR Study. (Class of as... -
Voltage-gated N-type calcium channel alpha-1B subunit/Amyloid beta A4 precursor protein-binding family A member 1 IC50 = 6910.0 nM 5.16 PUBCHEM_BIOASSAY: Homogeneous Time-Resolved Fluorescence Resonance Energy Transf... -
Dual specificity protein phosphatase 6 IC50 = 75200.0 nM 4.12 PUBCHEM_BIOASSAY: MKP-3 in vitro HTS assay. (Class of assay: confirmatory) [Rela... -

Data from ChEMBL 36 via Core Engine