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Compound Detail

CHEMBL1572266

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CS(=O)(=O)O.NC1C2CN(c3nc4c(cc3F)c(=O)c(C(=O)O)cn4-c3ccc(F)cc3F)CC12

Basic Information

ChEMBL ID CHEMBL1572266
Phase Preclinical
Structure Type MOL
InChI Key DYNZICQDCVYXFW-UHFFFAOYSA-N
Parent Compound CHEMBL1624529
Active Moiety CHEMBL1624529
7
Targets
19
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

416.4
MW (Da)
1.89
ALogP
6
HBA
2
HBD
101.5
PSA (Ų)
0.68
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H19F3N4O6S
MW 512.47
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.78

Activity Summary

EC50 11 meas. best 6.82
IC50 8 meas. best 6.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Streptokinase A
CHEMBL1293228
EC50 6.82 6.82 151.0 1
Streptococcus sp. 'group A'
CHEMBL612389
EC50 6.66 6.66 217.0 1
Streptococcus
CHEMBL612313
EC50 6.52 6.52 299.0 1
Unchecked
CHEMBL612545
IC50 6.46 6.1167 350.0 6
DNA damage-inducible transcript 3 protein
CHEMBL2146304
IC50 5.97 5.97 1080.0 1
Unchecked
CHEMBL612545
EC50 5.07 4.7943 8578.0 7
X-box-binding protein 1
CHEMBL1741176
IC50 5.0 5.0 10000.0 1
Nuclear factor NF-kappa-B complex
CHEMBL2094258
EC50 4.96 4.96 11094.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Streptokinase A EC50 = 151.0 nM 6.82 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptococcus sp. 'group A' EC50 = 217.0 nM 6.66 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Streptococcus EC50 = 299.0 nM 6.52 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... -
Unchecked IC50 = 350.0 nM 6.46 PUBCHEM_BIOASSAY: A screen for inhibitors of the PhoP region in Salmonella Typhi... -
Unchecked IC50 = 650.0 nM 6.19 PUBCHEM_BIOASSAY: A counter screen for small molecule screen for inhibitors of t... -
Unchecked IC50 = 720.0 nM 6.14 PUBCHEM_BIOASSAY: A screen for inhibitors of the PhoP region in Salmonella Typhi... -
Unchecked IC50 = 750.0 nM 6.12 PUBCHEM_BIOASSAY: A small molecule screen for inhibitors of the PhoP region in S... -
DNA damage-inducible transcript 3 protein IC50 = 1080.0 nM 5.97 PUBCHEM_BIOASSAY: CHOP dose-response primary assay. (Class of assay: confirmator... -
Unchecked IC50 = 1215.0 nM 5.92 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Inhibitors of Mycobacterium... -
Unchecked IC50 = 1340.0 nM 5.87 PUBCHEM_BIOASSAY: A Counter Screen to identiry small molecule screen for inhibit... -
Unchecked EC50 = 8578.0 nM 5.07 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Compounds that Suppress the... -
Unchecked EC50 = 8581.0 nM 5.07 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Compounds that Suppress the... -
X-box-binding protein 1 IC50 = 10000.0 nM 5.0 PUBCHEM_BIOASSAY: XBP1 DR counterscreen for CHOP. (Class of assay: confirmatory)... -
Nuclear factor NF-kappa-B complex EC50 = 11094.0 nM 4.96 PUBCHEM_BIOASSAY: Name: High Throughput Screen to Identify Compounds that increa... -
Unchecked EC50 = 15538.0 nM 4.81 PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Inhibito... -
Unchecked EC50 = 18550.0 nM 4.73 PUBCHEM_BIOASSAY: Fluorescent HTS Cytotoxicity/Cell viability assay (HPDE-C7 cel... -
Unchecked EC50 = 19220.0 nM 4.72 PUBCHEM_BIOASSAY: Fluorescent HTS Cytotoxicity/Cell viability assay (HPDE-C7K ce... -
Unchecked EC50 = 23080.0 nM 4.64 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Unchecked EC50 = 30060.0 nM 4.52 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -

Data from ChEMBL 36 via Core Engine