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Compound Detail

CHEMBL3356074

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COc1cccc2c1C(NCC(C)(C)c1ccccc1)=NC2=O

Basic Information

ChEMBL ID CHEMBL3356074
Phase Preclinical
Structure Type MOL
InChI Key WVNWIKASGFTXTN-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
2
PK Parameters
7
Publications
0
Known Names

Molecular Properties

308.4
MW (Da)
3.16
ALogP
3
HBA
1
HBD
50.7
PSA (Ų)
0.94
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 C19H20N2O2
MW 308.38
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -0.43

Activity Summary

IC50 2 meas. best 7.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Potassium voltage-gated channel subfamily A member 5
CHEMBL4306
IC50 7.47 7.275 34.0 2

Pharmacokinetic Data

Parameter Value Units Species
CL 35.0 mL.min-1.kg-1 Rattus norvegicus
T1/2 0.8 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24881565 10.1016/j.bmcl.2014.05.035 Rattus norvegicus 3
24881565 10.1016/j.bmcl.2014.05.035 ADMET 2
25801931 10.1016/j.bmcl.2015.02.066 Liver microsome 2
24881565 10.1016/j.bmcl.2014.05.035 Potassium voltage-gated channel subfamily A member 5 1
24881565 10.1016/j.bmcl.2014.05.035 Voltage-gated inwardly rectifying potassium channel KCNH2 1
25801931 10.1016/j.bmcl.2015.02.066 Potassium voltage-gated channel subfamily A member 5 1
25801931 10.1016/j.bmcl.2015.02.066 ADMET 1

Data from ChEMBL 36 via Core Engine