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Compound Detail

CHEMBL4062161

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CCN1CCc2c(sc(NC(=O)Nc3ccc(Cl)cc3)c2C(N)=O)C1.Cl

Basic Information

ChEMBL ID CHEMBL4062161
Phase Preclinical
Structure Type MOL
InChI Key JBFLYWJGBBWDIC-UHFFFAOYSA-N
Parent Compound CHEMBL4092306
Active Moiety CHEMBL4092306
2
Targets
2
Activities
2
Assay Types
2
PK Parameters
7
Publications
0
Known Names

Molecular Properties

378.9
MW (Da)
3.52
ALogP
4
HBA
3
HBD
87.5
PSA (Ų)
0.76
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H20Cl2N4O2S
MW 415.35
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -2.24

Activity Summary

EC50 1 meas. best 5.51
IC50 1 meas. best 5.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Danio rerio
CHEMBL613963
EC50 5.51 5.51 3120.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.49 5.49 3260.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 46.0 % Rattus norvegicus
T1/2 2.1 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28992413 10.1021/acs.jmedchem.7b00932 Rattus norvegicus 4
28992413 10.1021/acs.jmedchem.7b00932 Danio rerio 2
28992413 10.1021/acs.jmedchem.7b00932 Plasma 2
28992413 10.1021/acs.jmedchem.7b00932 Escherichia coli 2
28992413 10.1021/acs.jmedchem.7b00932 Voltage-gated inwardly rectifying potassium channel KCNH2 1
28992413 10.1021/acs.jmedchem.7b00932 HepG2 1
28992413 10.1021/acs.jmedchem.7b00932 No relevant target 1

Data from ChEMBL 36 via Core Engine