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Compound Detail

CHEMBL2151156

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CC1(C)CCCN(CCCOc2ccc(C3CCN(C(=O)c4ccc(CCC(=O)O)c5ccccc45)CC3)cc2)C1

Basic Information

ChEMBL ID CHEMBL2151156
Phase Preclinical
Structure Type MOL
InChI Key UZFUMFWJEGINFP-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

556.8
MW (Da)
6.77
ALogP
4
HBA
1
HBD
70.1
PSA (Ų)
0.28
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H44N2O4
MW 556.75
Aromatic Rings 3
Heavy Atoms 41
NP-Likeness -0.56

Activity Summary

Ki 2 meas. best 7.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL231
Ki 7.9 7.9 12.6 1
Histamine H3 receptor
CHEMBL264
Ki 7.3 7.3 50.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21062081 10.1021/jm100064d Cavia porcellus 2
21062081 10.1021/jm100064d Histamine H3 receptor 1
21062081 10.1021/jm100064d Histamine H1 receptor 1

Data from ChEMBL 36 via Core Engine