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Compound Detail

CHEMBL5087053

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CN1CCC(NC(=O)c2cccn3c(=O)c4ccc5ccccc5c4nc23)CC1

Basic Information

ChEMBL ID CHEMBL5087053
Phase Preclinical
Structure Type MOL
InChI Key GILGKICYVDVCLZ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

386.5
MW (Da)
2.82
ALogP
5
HBA
1
HBD
66.7
PSA (Ų)
0.42
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H22N4O2
MW 386.46
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.20

Activity Summary

IC50 1 meas. best 5.13

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.13 5.13 7390.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35450366 10.1021/acsmedchemlett.1c00660 Cytochrome P450 1A2 1
35450366 10.1021/acsmedchemlett.1c00660 DNA-directed RNA polymerase I subunit RPA1 1
35450366 10.1021/acsmedchemlett.1c00660 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine