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Compound Detail

CHEMBL3925332

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O=C(O)c1cc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2ncccc2c1

Basic Information

ChEMBL ID CHEMBL3925332
Phase Preclinical
Structure Type MOL
InChI Key JEMXPJDXKPVMFB-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

516.7
MW (Da)
4.94
ALogP
6
HBA
1
HBD
69.1
PSA (Ų)
0.38
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H40N4O3
MW 516.69
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -1.00

Activity Summary

IC50 1 meas. best 4.4
Ki 1 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL264
Ki 8.7 8.7 2.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 4.4 4.4 39810.7 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27866818 10.1016/j.bmcl.2016.11.022 Histamine H1 receptor 1
27866818 10.1016/j.bmcl.2016.11.022 Histamine H3 receptor 1
27866818 10.1016/j.bmcl.2016.11.022 Alpha-1A adrenergic receptor 1
27866818 10.1016/j.bmcl.2016.11.022 Alpha-1B adrenergic receptor 1
27866818 10.1016/j.bmcl.2016.11.022 No relevant target 1
27866818 10.1016/j.bmcl.2016.11.022 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine