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Compound Detail

CHEMBL203696

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FC1(F)CCN(Cc2ccc(OCCCN3CCC(Cc4c[nH]cn4)CC3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL203696
Phase Preclinical
Structure Type MOL
InChI Key XDGUQVBQTIPEEA-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

432.6
MW (Da)
4.36
ALogP
4
HBA
1
HBD
44.4
PSA (Ų)
0.60
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H34F2N4O
MW 432.56
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -0.92

Activity Summary

IC50 1 meas. best 5.22
Ki 1 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL5076
Ki 8.4 8.4 4.0 1
Cytochrome P450 2D6
CHEMBL289
IC50 5.22 5.22 6000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16297617 10.1016/j.bmcl.2005.10.087 Histamine H3 receptor 2
16297617 10.1016/j.bmcl.2005.10.087 Cytochrome P450 2D6 1

Data from ChEMBL 36 via Core Engine