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Compound Detail

CHEMBL3917794

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O=C(O)c1ccc2cccc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1

Basic Information

ChEMBL ID CHEMBL3917794
Phase Preclinical
Structure Type MOL
InChI Key VGLVSBTUAYHUEF-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
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 -0.96

Activity Summary

Ki 2 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL264
Ki 9.3 9.3 0.5 1
Histamine H1 receptor
CHEMBL231
Ki 6.6 6.6 251.2 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

Data from ChEMBL 36 via Core Engine