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Compound Detail

CHEMBL5426449

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CCc1ncc(-c2cc(C)no2)c(C2CCN(CCC(=O)N3CCOCC3)CC2)n1

Basic Information

ChEMBL ID CHEMBL5426449
Phase Preclinical
Structure Type MOL
InChI Key MKEDWZMIOHPVSV-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

413.5
MW (Da)
2.43
ALogP
7
HBA
0
HBD
84.6
PSA (Ų)
0.72
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H31N5O3
MW 413.52
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -1.95

Activity Summary

IC50 1 meas. best 5.35
Ki 1 meas. best 7.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sigma intracellular receptor 2
CHEMBL4105907
Ki 7.21 7.21 62.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.35 5.35 4500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
37607512 10.1021/acs.jmedchem.3c01060 ADMET 3
37607512 10.1021/acs.jmedchem.3c01060 Sigma non-opioid intracellular receptor 1 1
37607512 10.1021/acs.jmedchem.3c01060 Sigma intracellular receptor 2 1
37607512 10.1021/acs.jmedchem.3c01060 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine