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Compound Detail

CHEMBL3092826

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CC(C)NC(=O)c1ccc(Oc2ccc3c(c2)CCN(C2CCC2)CC3)nc1

Basic Information

ChEMBL ID CHEMBL3092826
Phase Preclinical
Structure Type MOL
InChI Key VZKZGBJWQULREW-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

379.5
MW (Da)
3.97
ALogP
4
HBA
1
HBD
54.5
PSA (Ų)
0.85
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 C23H29N3O2
MW 379.50
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -1.28

Activity Summary

Ki 2 meas. best 9.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL264
Ki 9.9 9.9 0.1 1
Histamine H3 receptor
CHEMBL4124
Ki 9.2 9.2 0.6 1

Pharmacokinetic Data

Parameter Value Units Species
CL 3.0 mL.min-1.g-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24269482 10.1016/j.bmcl.2013.09.090 Histamine H3 receptor 2
24269482 10.1016/j.bmcl.2013.09.090 Liver microsome 1
24269482 10.1016/j.bmcl.2013.09.090 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine