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Compound Detail

CHEMBL327888

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CCOCCn1c(C(=O)C2CCN(CCC3(c4ccc(OC)c(OC)c4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21

Basic Information

ChEMBL ID CHEMBL327888
Phase Preclinical
Structure Type MOL
InChI Key OEJHRMYSNOPXGZ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

728.9
MW (Da)
5.88
ALogP
11
HBA
0
HBD
113.8
PSA (Ų)
0.10
QED
3
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C41H52N4O8
MW 728.89
Aromatic Rings 4
Heavy Atoms 53
NP-Likeness -0.75

Activity Summary

IC50 2 meas. best 8.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL231
IC50 8.21 8.21 6.2 1
Substance-P receptor
CHEMBL3942
IC50 8.13 8.13 7.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histamine H1 receptor IC50 = 6.2 nM 8.21 Antagonistic activity against histamine H1 receptor -
Substance-P receptor IC50 = 7.39 nM 8.13 Antagonistic activity against Tachykinin receptor 1 -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(97)10098-1 Substance-P receptor 1
- 10.1016/S0960-894X(97)10098-1 Histamine H1 receptor 1

Data from ChEMBL 36 via Core Engine