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Compound Detail

CHEMBL3917428

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O=C(O)CCc1ccc2cc(Cc3ccccc3)cc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1

Basic Information

ChEMBL ID CHEMBL3917428
Phase Preclinical
Structure Type MOL
InChI Key FZTMDWIJTHPEMP-UHFFFAOYSA-N
5
Targets
6
Activities
3
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

634.9
MW (Da)
6.85
ALogP
6
HBA
1
HBD
69.1
PSA (Ų)
0.15
QED
2
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C40H50N4O3
MW 634.87
Aromatic Rings 4
Heavy Atoms 47
NP-Likeness -0.69

Activity Summary

Ki 4 meas. best 9.5
IC50 1 meas. best 5.2
Kd 1 meas. best 8.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL264
Ki 9.5 9.5 0.3 1
Histamine H1 receptor
CHEMBL231
Kd 8.2 8.2 6.3 1
Histamine H1 receptor
CHEMBL231
Ki 7.6 7.6 25.1 1
Alpha-1A adrenergic receptor
CHEMBL229
Ki 7.3 7.3 50.1 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 6.6 6.6 251.2 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.2 5.2 6309.6 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 4
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
27866818 10.1016/j.bmcl.2016.11.022 ADMET 1

Data from ChEMBL 36 via Core Engine