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Compound Detail

CHEMBL3286436

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COc1cc(C#N)c2ccc(=O)n(CCN3CCC(NCc4cnc(C)c(C#N)c4)CC3)c2c1

Basic Information

ChEMBL ID CHEMBL3286436
Phase Preclinical
Structure Type MOL
InChI Key LVXBUMWPFFTWIQ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
6
Publications
0
Known Names

Molecular Properties

456.6
MW (Da)
2.71
ALogP
8
HBA
1
HBD
107.0
PSA (Ų)
0.58
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 C26H28N6O2
MW 456.55
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.01

Activity Summary

IC50 2 meas. best 7.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA gyrase subunit A/DNA gyrase subunit B
CHEMBL3430898
IC50 7.19 7.19 65.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.6 5.6 2500.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 10.0 mL.min-1.kg-1 Rattus norvegicus
F 59.0 % Rattus norvegicus

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 Rattus norvegicus 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 No relevant target 1
24809953 10.1021/jm500432n Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine