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Compound Detail

CHEMBL1699206

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O=C(N/N=C/c1ccc(-c2ccc(S(=O)(=O)Nc3ncccn3)cc2)o1)c1cc2ccccc2cc1O

Basic Information

ChEMBL ID CHEMBL1699206
Phase Preclinical
Structure Type MOL
InChI Key RUMPAMJMDBPTGC-MUFRIFMGSA-N
9
Targets
11
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

513.5
MW (Da)
4.16
ALogP
8
HBA
3
HBD
146.8
PSA (Ų)
0.22
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H19N5O5S
MW 513.54
Aromatic Rings 5
Heavy Atoms 37
NP-Likeness -1.46

Activity Summary

IC50 11 meas. best 5.79

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Induced myeloid leukemia cell differentiation protein Mcl-1
CHEMBL4361
IC50 5.79 5.79 1632.8 1
SUMO-activating enzyme
CHEMBL2095174
IC50 5.66 5.285 2210.0 2
Envelope glycoprotein gp160
CHEMBL1293311
IC50 5.27 5.27 5360.0 1
Cysteine protease ATG4B
CHEMBL1741221
IC50 5.22 5.22 5980.0 1
Unchecked
CHEMBL612545
IC50 4.94 4.855 11400.0 2
Phospholipase A2
CHEMBL4426
IC50 4.69 4.69 20300.0 1
26S proteasome non-ATPase regulatory subunit 14
CHEMBL2007629
IC50 4.48 4.48 33300.0 1
Aminopeptidase N
CHEMBL4117
IC50 4.37 4.37 42330.0 1
Prothrombin
CHEMBL4471
IC50 4.12 4.12 75600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Induced myeloid leukemia cell differentiation protein Mcl-1 IC50 = 1632.75 nM 5.79 PUBCHEM_BIOASSAY: Dose Response Confirmation for Mcl-1/Noxa Interaction Inhibito... -
SUMO-activating enzyme IC50 = 2210.0 nM 5.66 PUBCHEM_BIOASSAY: AlphaScreen confirmatory assay for validation of inhibitors of... -
Envelope glycoprotein gp160 IC50 = 5360.0 nM 5.27 PUBCHEM_BIOASSAY: uHTS fluorescence assay for the identification of Human Immuno... -
Cysteine protease ATG4B IC50 = 5980.0 nM 5.22 PUBCHEM_BIOASSAY: Dose response confirmation of the uHTS fluorescent assay for i... -
Unchecked IC50 = 11400.0 nM 4.94 PubChem BioAssay. Dose Response confirmation of small molecule inhibitors origin... -
SUMO-activating enzyme IC50 = 12400.0 nM 4.91 PUBCHEM_BIOASSAY: uHTS HTRF assay for identification of inhibitors of SUMOylatio... -
Unchecked IC50 = 17000.0 nM 4.77 PUBCHEM_BIOASSAY: A Cell Based Assay for the Identification of Lead Compounds wi... -
Phospholipase A2 IC50 = 20300.0 nM 4.69 PUBCHEM_BIOASSAY: Dose response counterscreen of uHTS hits for ATG4B inhibitors ... -
26S proteasome non-ATPase regulatory subunit 14 IC50 = 33300.0 nM 4.48 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS RPN11 inhibitor hits in a F... -
Aminopeptidase N IC50 = 42330.0 nM 4.37 PUBCHEM_BIOASSAY: Inhibitors of Plasmodium falciparum M1- Family Alanyl Aminopep... -
Prothrombin IC50 = 75600.0 nM 4.12 PUBCHEM_BIOASSAY: Dose Response validation of uHTS RPN11 inhibitor hits using a ... -

Data from ChEMBL 36 via Core Engine