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Compound Detail

CHEMBL1521960

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CN1/C(=C\C=C\C2=[N+](C)c3ccc4ccccc4c3C2(C)C)C(C)(C)c2ccccc21.[O-][Cl+3]([O-])([O-])[O-]

Basic Information

ChEMBL ID CHEMBL1521960
Phase Preclinical
Structure Type MOL
InChI Key TUROROWBICYGHB-UHFFFAOYSA-M
Parent Compound CHEMBL600519
Active Moiety CHEMBL600519
6
Targets
15
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

407.6
MW (Da)
6.71
ALogP
1
HBA
0
HBD
6.2
PSA (Ų)
0.43
QED
1
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H31ClN2O4
MW 507.03
Aromatic Rings 3
Heavy Atoms 31

Activity Summary

IC50 9 meas. best 6.8
EC50 6 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 8.4 7.3067 4.0 3
X-box-binding protein 1
CHEMBL1741176
IC50 6.8 6.8 160.0 1
Unchecked
CHEMBL612545
IC50 6.12 5.2457 761.4 7
Nucleic Acid
CHEMBL345
EC50 5.33 5.33 4710.0 1
Ephrin type-A receptor 4
CHEMBL1293259
IC50 5.3 5.3 4950.0 1
Peroxisome proliferator-activated receptor gamma/Nuclear receptor coactivator 2
CHEMBL2095163
EC50 5.09 5.09 8191.0 1
Peroxisome proliferator-activated receptor gamma/Nuclear receptor coactivator 1
CHEMBL2095162
EC50 4.87 4.87 13380.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 4.0 nM 8.4 PubChem BioAssay. Leishmania major promastigote EC50 determinations. (Class of... -
Unchecked EC50 = 150.0 nM 6.82 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
X-box-binding protein 1 IC50 = 160.0 nM 6.8 PUBCHEM_BIOASSAY: XBP1 DR counterscreen for CHOP. (Class of assay: confirmatory)... -
Unchecked EC50 = 200.0 nM 6.7 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Unchecked IC50 = 761.42 nM 6.12 PUBCHEM_BIOASSAY: Luminescence-based dose response cell-based high throughput sc... -
Unchecked IC50 = 3618.0 nM 5.44 PUBCHEM_BIOASSAY: A screen for inhibitors of the PhoP region in Salmonella Typhi... -
Nucleic Acid EC50 = 4710.0 nM 5.33 PUBCHEM_BIOASSAY: Luminescent HTS for small molecule inhibitors of MT1-MMP trans... -
Ephrin type-A receptor 4 IC50 = 4950.0 nM 5.3 PUBCHEM_BIOASSAY: Colorimetric assay for HTS discovery of chemical inhibitors of... -
Unchecked IC50 = 5780.0 nM 5.24 PUBCHEM_BIOASSAY: A small molecule screen for inhibitors of the PhoP region in S... -
Peroxisome proliferator-activated receptor gamma/Nuclear receptor coactivator 2 EC50 = 8191.0 nM 5.09 PUBCHEM_BIOASSAY: TR-FRET dose response biochemical High Throughput Screening as... -
Unchecked IC50 = 8850.0 nM 5.05 PUBCHEM_BIOASSAY: A counter screen for small molecule screen for inhibitors of t... -
Unchecked IC50 = 9420.0 nM 5.03 PUBCHEM_BIOASSAY: A Counter Screen to identiry small molecule screen for inhibit... -
Unchecked IC50 = 10180.0 nM 4.99 PUBCHEM_BIOASSAY: A small molecule screen for inhibitors of the PhoP region in S... -
Peroxisome proliferator-activated receptor gamma/Nuclear receptor coactivator 1 EC50 = 13380.0 nM 4.87 PUBCHEM_BIOASSAY: TR-FRET dose response biochemical High Throughput Screening as... -
Unchecked IC50 = 14120.0 nM 4.85 PUBCHEM_BIOASSAY: A screen for inhibitors of the PhoP region in Salmonella Typhi... -

Data from ChEMBL 36 via Core Engine