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Compound Detail

CHEMBL3752972

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COc1ccc(CNc2nc3c(c(N4CCN(C)CC4)n2)-c2ccccc2CC3)cc1

Basic Information

ChEMBL ID CHEMBL3752972
Phase Preclinical
Structure Type MOL
InChI Key VMWDGVHSQTWDFE-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

415.5
MW (Da)
3.61
ALogP
6
HBA
1
HBD
53.5
PSA (Ų)
0.69
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H29N5O
MW 415.54
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.89

Activity Summary

Ki 2 meas. best 5.97

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL231
Ki 5.97 5.97 1071.5 1
Histamine H4 receptor
CHEMBL3759
Ki 4.86 4.86 13803.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26718844 10.1016/j.bmcl.2015.12.035 Histamine H1 receptor 1
26718844 10.1016/j.bmcl.2015.12.035 Histamine H4 receptor 1

Data from ChEMBL 36 via Core Engine