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Compound Detail

CHEMBL3298226

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COc1cccc2ccnc(NCC(C)(C)c3ccccc3)c12

Basic Information

ChEMBL ID CHEMBL3298226
Phase Preclinical
Structure Type MOL
InChI Key WZDLNTAETYKZDN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

306.4
MW (Da)
4.63
ALogP
3
HBA
1
HBD
34.1
PSA (Ų)
0.75
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H22N2O
MW 306.41
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -0.66

Activity Summary

IC50 1 meas. best 7.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Potassium voltage-gated channel subfamily A member 5
CHEMBL4306
IC50 7.66 7.66 22.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 124.0 mL.min-1.kg-1 Rattus norvegicus
T1/2 1.8 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 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
24881565 10.1016/j.bmcl.2014.05.035 ADMET 1

Data from ChEMBL 36 via Core Engine