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Compound Detail

CHEMBL3290336

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COc1ccc2ccc(=O)n(CCN3CCC(NCc4ccc5c(n4)NC(=O)CO5)CC3)c2n1

Basic Information

ChEMBL ID CHEMBL3290336
Phase Preclinical
Structure Type MOL
InChI Key NBGOQUKSSZOVOU-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

464.5
MW (Da)
1.39
ALogP
9
HBA
2
HBD
110.6
PSA (Ų)
0.54
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H28N6O4
MW 464.53
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.19

Activity Summary

IC50 3 meas. best 6.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA gyrase subunit A/DNA gyrase subunit B
CHEMBL3430898
IC50 6.82 6.82 150.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 4.68 4.66 21000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24809953 10.1021/jm500432n Caco-2 2
24809953 10.1021/jm500432n Mycobacterium tuberculosis 1
24809953 10.1021/jm500432n DNA gyrase subunit A/DNA gyrase subunit B 1
24809953 10.1021/jm500432n DNA gyrase subunit B 1
24809953 10.1021/jm500432n No relevant target 1
24809953 10.1021/jm500432n Voltage-gated inwardly rectifying potassium channel KCNH2 1
26191359 10.1021/ml500531p Mycobacterium tuberculosis 1
26191359 10.1021/ml500531p Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine