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Compound Detail

CHEMBL3590499

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COc1ccc(-c2ccc(C#Cc3cccc(C#Cc4ccc(-c5ccc(OC)cc5)cc4)[n+]3C)cc2)cc1.O=S(=O)([O-])C(F)(F)F

Basic Information

ChEMBL ID CHEMBL3590499
Phase Preclinical
Structure Type MOL
InChI Key HKICHFGDUNWGML-UHFFFAOYSA-M
Parent Compound CHEMBL3590678
Active Moiety CHEMBL3590678
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

506.6
MW (Da)
6.66
ALogP
2
HBA
0
HBD
22.3
PSA (Ų)
0.20
QED
2
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C37H28F3NO5S
MW 655.69
Aromatic Rings 5
Heavy Atoms 39
NP-Likeness -0.15

Activity Summary

Kd 1 meas. best 6.98
Ki 1 meas. best 6.61

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
Kd 6.98 6.98 105.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
Ki 6.61 6.61 247.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26125327 10.1021/acs.jmedchem.5b00518 Voltage-gated inwardly rectifying potassium channel KCNH2 5

Data from ChEMBL 36 via Core Engine