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Compound Detail

CHEMBL3215681

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CC(C)n1nc(C(=O)NCC2CCN(CCN3CCOCC3)CC2)c2ccccc21.Cl.Cl

Basic Information

ChEMBL ID CHEMBL3215681
Phase Preclinical
Structure Type MOL
InChI Key FBJBOIWNNPBFCD-UHFFFAOYSA-N
Parent Compound CHEMBL2220906
Active Moiety CHEMBL2220906
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

413.6
MW (Da)
2.39
ALogP
6
HBA
1
HBD
62.6
PSA (Ų)
0.76
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H37Cl2N5O2
MW 486.49
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -1.49

Activity Summary

IC50 1 meas. best 4.49
Ki 1 meas. best 9.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 4
CHEMBL1875
Ki 9.4 9.4 0.4 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 4.49 4.49 32500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23043420 10.1021/jm300573d Voltage-gated inwardly rectifying potassium channel KCNH2 2
23043420 10.1021/jm300573d 5-hydroxytryptamine receptor 2A 1
23043420 10.1021/jm300573d 5-hydroxytryptamine receptor 4 1

Data from ChEMBL 36 via Core Engine