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Compound Detail

CHEMBL1566994

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COc1cc(NS(=O)(=O)c2ccc(NC(=S)NC(=O)/C=C/c3ccco3)cc2)ncn1

Basic Information

ChEMBL ID CHEMBL1566994
Phase Preclinical
Structure Type MOL
InChI Key PPYMPELJQZQIBQ-RMKNXTFCSA-N
10
Targets
11
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

459.5
MW (Da)
2.41
ALogP
8
HBA
3
HBD
135.4
PSA (Ų)
0.36
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 C19H17N5O5S2
MW 459.51
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -2.05

Activity Summary

IC50 11 meas. best 5.67

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
IC50 5.67 5.67 2150.0 1
SUMO-activating enzyme
CHEMBL2095174
IC50 5.62 5.1 2410.0 2
DNA (cytosine-5)-methyltransferase 1
CHEMBL1993
IC50 5.54 5.54 2920.0 1
Cysteine protease ATG4B
CHEMBL1741221
IC50 5.22 5.22 6000.0 1
26S proteasome non-ATPase regulatory subunit 14
CHEMBL2007629
IC50 4.89 4.89 12900.0 1
Intestinal-type alkaline phosphatase
CHEMBL3151
IC50 4.74 4.74 18400.0 1
Prothrombin
CHEMBL4471
IC50 4.69 4.69 20500.0 1
Tyrosyl-DNA phosphodiesterase 2
CHEMBL2169736
IC50 4.52 4.52 30397.0 1
Alkaline phosphatase, tissue-nonspecific isozyme
CHEMBL5979
IC50 4.34 4.34 45900.0 1
Alkaline phosphatase, germ cell type
CHEMBL3402
IC50 4.26 4.26 55100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
72 kDa type IV collagenase IC50 = 2150.0 nM 5.67 PUBCHEM_BIOASSAY: Dose Response validation of uHTS RPN11 inhibitor hits using a ... -
SUMO-activating enzyme IC50 = 2410.0 nM 5.62 PUBCHEM_BIOASSAY: AlphaScreen confirmatory assay for validation of inhibitors of... -
DNA (cytosine-5)-methyltransferase 1 IC50 = 2920.0 nM 5.54 PUBCHEM_BIOASSAY: Dose response confirmation of DNMT1 inhibitors in a Fluorescen... -
Cysteine protease ATG4B IC50 = 6000.0 nM 5.22 PUBCHEM_BIOASSAY: Dose response confirmation of the uHTS fluorescent assay for i... -
26S proteasome non-ATPase regulatory subunit 14 IC50 = 12900.0 nM 4.89 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS RPN11 inhibitor hits in a F... -
Intestinal-type alkaline phosphatase IC50 = 18400.0 nM 4.74 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS hits from a small molecule ... -
Prothrombin IC50 = 20500.0 nM 4.69 PUBCHEM_BIOASSAY: Dose Response validation of uHTS RPN11 inhibitor hits using a ... -
SUMO-activating enzyme IC50 = 26110.0 nM 4.58 PUBCHEM_BIOASSAY: uHTS HTRF assay for identification of inhibitors of SUMOylatio... -
Tyrosyl-DNA phosphodiesterase 2 IC50 = 30397.0 nM 4.52 PubChem BioAssay. Epi Absorbance-based biochemical high throughput dose response... -
Alkaline phosphatase, tissue-nonspecific isozyme IC50 = 45900.0 nM 4.34 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS inhibitors of Mouse Intesti... -
Alkaline phosphatase, germ cell type IC50 = 55100.0 nM 4.26 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS inhibitors of Mouse Intesti... -

Data from ChEMBL 36 via Core Engine