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Compound Detail

CHEMBL487265

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O=C(CO)N1C[C@@H]2CC=C(c3ccc(CCN4CCCC4)cc3)[C@@H]2C1

Basic Information

ChEMBL ID CHEMBL487265
Phase Preclinical
Structure Type MOL
InChI Key IEKCOXKNCRBHNT-AZUAARDMSA-N
1
Targets
2
Activities
1
Assay Types
3
PK Parameters
2
Publications
0
Known Names

Molecular Properties

340.5
MW (Da)
2.18
ALogP
3
HBA
1
HBD
43.8
PSA (Ų)
0.89
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 C21H28N2O2
MW 340.47
Aromatic Rings 1
Heavy Atoms 25
NP-Likeness -0.07

Activity Summary

Ki 2 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL4124
Ki 8.22 8.21 6.0 2

Pharmacokinetic Data

Parameter Value Units Species
F 39.0 % Rattus norvegicus
T1/2 1.8 hr Rattus norvegicus
Tmax 0.6 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18554904 10.1016/j.bmcl.2008.05.086 Rattus norvegicus 3
18554904 10.1016/j.bmcl.2008.05.086 Histamine H3 receptor 2

Data from ChEMBL 36 via Core Engine