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Compound Detail

CHEMBL316705

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COC(=O)c1ccccc1OCCCn1c(C(=O)C2CCN(CCC3(c4ccccc4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21

Basic Information

ChEMBL ID CHEMBL316705
Phase Preclinical
Structure Type MOL
InChI Key ZFPPUHTZTYNOKP-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

788.9
MW (Da)
7.09
ALogP
11
HBA
0
HBD
121.7
PSA (Ų)
0.06
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 C46H52N4O8
MW 788.94
Aromatic Rings 5
Heavy Atoms 58
NP-Likeness -0.75

Activity Summary

IC50 2 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL3942
IC50 7.8 7.8 16.0 1
Histamine H1 receptor
CHEMBL231
IC50 6.0 6.0 994.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor IC50 = 16.0 nM 7.8 Antagonism of the guinea pig tachykinin NK1 receptor -
Histamine H1 receptor IC50 = 994.0 nM 6.0 Antagonism of the human histamine H1 receptor -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(97)10097-X Histamine H1 receptor 1
- 10.1016/S0960-894X(97)10097-X Substance-P receptor 1

Data from ChEMBL 36 via Core Engine