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Compound Detail

CHEMBL498260

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N#Cc1ccc2cc1Oc1ccc3cccc(c3c1)N1CC[C@@H](NCCc3cncn3C2)C1=O

Basic Information

ChEMBL ID CHEMBL498260
Phase Preclinical
Structure Type MOL
InChI Key OBXLXUGOZZWQOW-XMMPIXPASA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

449.5
MW (Da)
4.00
ALogP
6
HBA
1
HBD
83.2
PSA (Ų)
0.44
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H23N5O2
MW 449.51
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness 0.20

Activity Summary

IC50 2 meas. best 6.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 6.68 6.68 210.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19534531 10.1021/jm900002x Voltage-gated inwardly rectifying potassium channel KCNH2 1
- 10.1039/C2MD20010D Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine