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Compound Detail

CHEMBL1969046

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Cc1ccc(S(=O)(=O)/N=C2\C=C(Nc3cccc(C(=O)O)c3)C(=O)c3ccccc32)c(C)c1

Basic Information

ChEMBL ID CHEMBL1969046
Phase Preclinical
Structure Type MOL
InChI Key RUWHEBZPTCVEMQ-SZXQPVLSSA-N
16
Targets
19
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

460.5
MW (Da)
4.37
ALogP
5
HBA
2
HBD
112.9
PSA (Ų)
0.58
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H20N2O5S
MW 460.51
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.93

Activity Summary

IC50 16 meas. best 6.09
EC50 3 meas. best 4.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sentrin-specific protease 6
CHEMBL1741215
IC50 6.09 6.09 819.0 1
Heat shock protein HSP 90-alpha
CHEMBL3880
IC50 6.04 6.04 919.0 1
Unchecked
CHEMBL612545
IC50 6.01 5.6733 973.0 3
Sentrin-specific protease 8
CHEMBL1741207
IC50 5.75 5.75 1780.0 1
Tyrosyl-DNA phosphodiesterase 2
CHEMBL2169736
IC50 5.59 5.59 2575.0 1
Sentrin-specific protease 7
CHEMBL1741213
IC50 5.48 5.48 3300.0 1
Apoptotic protease-activating factor 1
CHEMBL1795093
IC50 5.39 5.39 4110.0 1
Hexokinase HKDC1
CHEMBL1741200
IC50 5.07 5.015 8600.0 2
Caspase-3
CHEMBL2334
IC50 4.95 4.95 11200.0 1
Serine/threonine-protein phosphatase
CHEMBL1293265
IC50 4.91 4.91 12272.0 1
Protein RecA
CHEMBL1741171
EC50 4.82 4.82 15000.0 1
Serine/threonine-protein phosphatase PP1-alpha catalytic subunit
CHEMBL2164
IC50 4.57 4.57 27075.0 1
Zinc finger protein mex-5
CHEMBL1293319
EC50 4.5 4.5 31700.0 1
C-C chemokine receptor type 6
CHEMBL4423
IC50 4.4 4.4 39900.0 1
Beta-galactosidase
CHEMBL1293264
IC50 4.36 4.36 43500.0 1
RNA-binding protein pos-1
CHEMBL1293304
EC50 4.16 4.16 68583.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sentrin-specific protease 6 IC50 = 819.0 nM 6.09 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
Heat shock protein HSP 90-alpha IC50 = 919.0 nM 6.04 PUBCHEM_BIOASSAY: Luminescence-based dose response biochemical high throughput s... -
Unchecked IC50 = 973.0 nM 6.01 PubChem BioAssay. Fluorescence-based biochemical high throughput screening dose ... -
Sentrin-specific protease 8 IC50 = 1780.0 nM 5.75 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
Unchecked IC50 = 2359.0 nM 5.63 PubChem BioAssay. Counterscreen for inhibitors of Crimean-Congo Hemorrhagic Feve... -
Tyrosyl-DNA phosphodiesterase 2 IC50 = 2575.0 nM 5.59 PubChem BioAssay. Epi Absorbance-based biochemical high throughput dose response... -
Sentrin-specific protease 7 IC50 = 3300.0 nM 5.48 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
Apoptotic protease-activating factor 1 IC50 = 4110.0 nM 5.39 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 in a Fluore... -
Unchecked IC50 = 4150.0 nM 5.38 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 using a LZ-... -
Hexokinase HKDC1 IC50 = 8600.0 nM 5.07 PUBCHEM_BIOASSAY: Dose Response confirmation of inhibitors of hexokinase domain ... -
Hexokinase HKDC1 IC50 = 11000.0 nM 4.96 PUBCHEM_BIOASSAY: Dose Response confirmation of inhibitors of hexokinase domain ... -
Caspase-3 IC50 = 11200.0 nM 4.95 PUBCHEM_BIOASSAY: Dose Response confirmation of inhibitors of Sentrin-specific p... -
Serine/threonine-protein phosphatase IC50 = 12272.0 nM 4.91 PUBCHEM_BIOASSAY: Fluorescence-based biochemical high throughput dose response a... -
Protein RecA EC50 = 15000.0 nM 4.82 PUBCHEM_BIOASSAY: Fluorescence Cell-Free Homogeneous Dose Retest to Identify Inh... -
Serine/threonine-protein phosphatase PP1-alpha catalytic subunit IC50 = 27075.0 nM 4.57 PUBCHEM_BIOASSAY: Counterscreen for inhibitors of PP5: fluorescence-based bioche... -
Zinc finger protein mex-5 EC50 = 31700.0 nM 4.5 PUBCHEM_BIOASSAY: Fluorescent Polarization Homogeneous Dose Response HTS to Iden... -
C-C chemokine receptor type 6 IC50 = 39900.0 nM 4.4 PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of th... -
Beta-galactosidase IC50 = 43500.0 nM 4.36 PUBCHEM_BIOASSAY: HTS Dose response counterscreen for assays utilizing the enzym... -
RNA-binding protein pos-1 EC50 = 68583.0 nM 4.16 PUBCHEM_BIOASSAY: Fluorescent Polarization Homogeneous Dose Response HTS to Iden... -

Data from ChEMBL 36 via Core Engine