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Compound Detail

CHEMBL3094128

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O=C(N[C@H]1CCN(Cc2ccc(OCCCN3CCCCC3)cc2)C1)c1ccc2c(c1)OCO2

Basic Information

ChEMBL ID CHEMBL3094128
Phase Preclinical
Structure Type MOL
InChI Key AVVIXBQVVAAVHK-QHCPKHFHSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

465.6
MW (Da)
3.67
ALogP
6
HBA
1
HBD
63.3
PSA (Ų)
0.57
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 C27H35N3O4
MW 465.59
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -1.35

Activity Summary

Ki 1 meas. best 10.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL264
Ki 10.6 10.6 0.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histamine H3 receptor Ki = 0.02512 nM 10.6 Antagonist activity at human histamine H3 receptor expressed in CHOK1 cells asse... 24161834

Literature References

PubMed DOI Target Context # Activities
24161834 10.1016/j.bmcl.2013.09.089 Rattus norvegicus 1
24161834 10.1016/j.bmcl.2013.09.089 Albumin 1
24161834 10.1016/j.bmcl.2013.09.089 Histamine H1 receptor 1
24161834 10.1016/j.bmcl.2013.09.089 Histamine H3 receptor 1

Data from ChEMBL 36 via Core Engine