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Compound Detail

CHEMBL1589425

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CCCCCCCCCC[N+](C)(C)CC/C=C1/c2ccccc2Sc2ccc(Cl)cc21.[Br-]

Basic Information

ChEMBL ID CHEMBL1589425
Phase Preclinical
Structure Type MOL
InChI Key DXLHUHJKEMQMBH-PNNXLEGYSA-M
Parent Compound CHEMBL1625287
Active Moiety CHEMBL1625287
9
Targets
20
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

457.1
MW (Da)
8.84
ALogP
1
HBA
0
HBD
0.0
PSA (Ų)
0.19
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H39BrClNS
MW 537.05
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -0.18

Activity Summary

IC50 13 meas. best 5.42
EC50 7 meas. best 5.78

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 5.78 5.74 1670.0 2
Streptococcus sp. 'group A'
CHEMBL612389
EC50 5.76 5.76 1746.0 1
Streptokinase A
CHEMBL1293228
EC50 5.64 5.41 2314.0 2
Ubiquitin-conjugating enzyme E2 N
CHEMBL6089
IC50 5.42 5.38 3770.0 2
Streptococcus
CHEMBL612313
EC50 5.25 5.25 5624.0 1
Protein RecA
CHEMBL1741171
EC50 5.24 5.24 5800.0 1
Bcl-2-related protein A1
CHEMBL1293239
IC50 5.09 5.09 8080.0 1
Apoptotic protease-activating factor 1
CHEMBL1795093
IC50 4.97 4.97 10600.0 1
Unchecked
CHEMBL612545
IC50 4.88 4.7288 13220.0 8
Melanocortin receptor 4
CHEMBL259
IC50 4.51 4.51 31201.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 1670.0 nM 5.78 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Streptococcus sp. 'group A' EC50 = 1746.0 nM 5.76 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Unchecked EC50 = 1990.0 nM 5.7 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Streptokinase A EC50 = 2314.0 nM 5.64 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Iden... -
Ubiquitin-conjugating enzyme E2 N IC50 = 3770.0 nM 5.42 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for the identification of U... -
Ubiquitin-conjugating enzyme E2 N IC50 = 4614.0 nM 5.34 PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for the identification of U... -
Streptococcus EC50 = 5624.0 nM 5.25 PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify... -
Protein RecA EC50 = 5800.0 nM 5.24 PUBCHEM_BIOASSAY: Fluorescence Cell-Free Homogeneous Dose Retest to Identify Inh... -
Streptokinase A EC50 = 6634.0 nM 5.18 PUBCHEM_BIOASSAY: Absorbance Microorganism-Based Dose Response HTS to Identify I... -
Bcl-2-related protein A1 IC50 = 8080.0 nM 5.09 PUBCHEM_BIOASSAY: Dose Response confirmation of UBC13 Polyubiquitin Inhibitors u... -
Apoptotic protease-activating factor 1 IC50 = 10600.0 nM 4.97 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 in a Fluore... -
Unchecked IC50 = 13220.0 nM 4.88 PUBCHEM_BIOASSAY: A small molecule screen for inhibitors of the PhoP region in S... -
Unchecked IC50 = 14000.0 nM 4.85 PUBCHEM_BIOASSAY: A counter screen for small molecule screen for inhibitors of t... -
Unchecked IC50 = 15200.0 nM 4.82 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 using a LZ-... -
Unchecked IC50 = 16467.0 nM 4.78 PUBCHEM_BIOASSAY: A screen for inhibitors of the PhoP region in Salmonella Typhi... -
Unchecked IC50 = 18470.0 nM 4.73 PUBCHEM_BIOASSAY: A small molecule screen for inhibitors of the PhoP region in S... -
Unchecked IC50 = 18890.0 nM 4.72 PUBCHEM_BIOASSAY: A Counter Screen to identiry small molecule screen for inhibit... -
Unchecked IC50 = 22598.0 nM 4.65 PUBCHEM_BIOASSAY: Counterscreen for biased ligands (antagonists) of the melanoco... -
Melanocortin receptor 4 IC50 = 31201.0 nM 4.51 PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay fo... -
Unchecked IC50 = 39950.0 nM 4.4 PUBCHEM_BIOASSAY: A screen for inhibitors of the PhoP region in Salmonella Typhi... -

Data from ChEMBL 36 via Core Engine