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Compound Detail

CHEMBL1608106

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O=C(O)CCn1cc(/C=C/C(=O)c2ccc(Cl)cc2)c(-c2cccc(Br)c2)n1

Basic Information

ChEMBL ID CHEMBL1608106
Phase Preclinical
Structure Type MOL
InChI Key PYTRNXVWUCEWPD-RMKNXTFCSA-N
8
Targets
12
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

459.7
MW (Da)
5.34
ALogP
4
HBA
1
HBD
72.2
PSA (Ų)
0.38
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 C21H16BrClN2O3
MW 459.73
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.26

Activity Summary

IC50 7 meas. best 5.39
EC50 5 meas. best 6.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Streptokinase A
CHEMBL1293228
EC50 6.06 5.745 874.0 2
HEK293
CHEMBL614818
IC50 5.39 5.0367 4060.0 3
Streptococcus sp. 'group A'
CHEMBL612389
EC50 5.36 5.36 4349.0 1
HEK293
CHEMBL614818
EC50 5.19 5.19 6520.0 1
Streptococcus
CHEMBL612313
EC50 5.17 5.17 6688.0 1
Phospholipase A2
CHEMBL4426
IC50 5.06 5.06 8650.0 1
Cysteine protease ATG4B
CHEMBL1741221
IC50 4.87 4.87 13500.0 1
Unchecked
CHEMBL612545
IC50 4.56 4.56 27820.0 1
Envelope glycoprotein gp160
CHEMBL1293311
IC50 4.55 4.55 28000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Streptokinase A EC50 = 874.0 nM 6.06 PUBCHEM_BIOASSAY: Absorbance Microorganism-Based Dose Response HTS to Identify I... -
Streptokinase A EC50 = 3680.0 nM 5.43 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
HEK293 IC50 = 4060.0 nM 5.39 PUBCHEM_BIOASSAY: uHTS luminescence assay for the identification of compounds th... -
Streptococcus sp. 'group A' EC50 = 4349.0 nM 5.36 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
HEK293 EC50 = 6520.0 nM 5.19 PUBCHEM_BIOASSAY: uHTS luminescence assay for the identification of compounds th... -
Streptococcus EC50 = 6688.0 nM 5.17 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... -
Phospholipase A2 IC50 = 8650.0 nM 5.06 PUBCHEM_BIOASSAY: Dose response counterscreen of uHTS hits for ATG4B inhibitors ... -
HEK293 IC50 = 10640.0 nM 4.97 PUBCHEM_BIOASSAY: HTS dose response assay for identification of inhibitors of TN... -
Cysteine protease ATG4B IC50 = 13500.0 nM 4.87 PUBCHEM_BIOASSAY: Dose response confirmation of the uHTS fluorescent assay for i... -
HEK293 IC50 = 17894.11 nM 4.75 PUBCHEM_BIOASSAY: uHTS Fluorescence assay for the identification of cytotoxic co... -
Unchecked IC50 = 27820.0 nM 4.56 PUBCHEM_BIOASSAY: A Cell Based Assay for the Identification of Lead Compounds wi... -
Envelope glycoprotein gp160 IC50 = 28000.0 nM 4.55 PUBCHEM_BIOASSAY: uHTS fluorescence assay for the identification of Human Immuno... -

Data from ChEMBL 36 via Core Engine