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Compound Detail

CHEMBL2000196

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CC(=O)N(/N=C1\Sc2ccccc2C1=O)c1ccccc1C

Basic Information

ChEMBL ID CHEMBL2000196
Phase Preclinical
Structure Type MOL
InChI Key OBPOWEVMSNKZCM-ZCXUNETKSA-N
9
Targets
14
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

310.4
MW (Da)
3.65
ALogP
4
HBA
0
HBD
49.7
PSA (Ų)
0.80
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H14N2O2S
MW 310.38
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -0.78

Activity Summary

IC50 12 meas. best 5.72
EC50 2 meas. best 5.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sentrin-specific protease 6
CHEMBL1741215
IC50 5.72 5.72 1910.0 1
Unchecked
CHEMBL612545
EC50 5.6 5.6 2510.0 1
Sentrin-specific protease 8
CHEMBL1741207
IC50 5.46 5.46 3460.0 1
Sentrin-specific protease 7
CHEMBL1741213
IC50 5.42 5.42 3790.0 1
NACHT, LRR and PYD domains-containing protein 3
CHEMBL1741208
IC50 5.34 5.21 4550.0 2
Apoptotic protease-activating factor 1
CHEMBL1795093
IC50 5.29 5.29 5130.0 1
Unchecked
CHEMBL612545
IC50 5.19 4.81 6500.0 4
Tyrosyl-DNA phosphodiesterase 2
CHEMBL2169736
IC50 5.12 5.12 7665.0 1
H4
CHEMBL1075452
EC50 4.48 4.48 33380.0 1
Caspase-3
CHEMBL2334
IC50 4.38 4.38 42200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sentrin-specific protease 6 IC50 = 1910.0 nM 5.72 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
Unchecked EC50 = 2510.0 nM 5.6 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Acti... -
Sentrin-specific protease 8 IC50 = 3460.0 nM 5.46 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
Sentrin-specific protease 7 IC50 = 3790.0 nM 5.42 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-s... -
NACHT, LRR and PYD domains-containing protein 3 IC50 = 4550.0 nM 5.34 PUBCHEM_BIOASSAY: Dose Response confirmation of inhibitors of NALP3 in yeast usi... -
Apoptotic protease-activating factor 1 IC50 = 5130.0 nM 5.29 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 in a Fluore... -
Unchecked IC50 = 6500.0 nM 5.19 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 using a LZ-... -
Unchecked IC50 = 7400.0 nM 5.13 PubChem BioAssay. Dose Response confirmation of small molecule inhibitors origin... -
Tyrosyl-DNA phosphodiesterase 2 IC50 = 7665.0 nM 5.12 PubChem BioAssay. Epi Absorbance-based biochemical high throughput dose response... -
NACHT, LRR and PYD domains-containing protein 3 IC50 = 8340.0 nM 5.08 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for the identification of i... -
Unchecked IC50 = 16520.0 nM 4.78 PubChem BioAssay. Fluorescence-based biochemical high throughput screening dose ... -
H4 EC50 = 33380.0 nM 4.48 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Activato... -
Caspase-3 IC50 = 42200.0 nM 4.38 PUBCHEM_BIOASSAY: Dose Response confirmation of inhibitors of Sentrin-specific p... -
Unchecked IC50 = 72968.0 nM 4.14 PubChem BioAssay. Counterscreen for inhibitors of Crimean-Congo Hemorrhagic Feve... -

Data from ChEMBL 36 via Core Engine