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Compound Detail

CHEMBL319535

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CC(C)Oc1cccc(CC(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)c1

Basic Information

ChEMBL ID CHEMBL319535
Phase Preclinical
Structure Type MOL
InChI Key GHVPKFCDNOFWEW-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

730.9
MW (Da)
7.44
ALogP
8
HBA
0
HBD
86.1
PSA (Ų)
0.12
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C44H47FN4O5
MW 730.88
Aromatic Rings 5
Heavy Atoms 54
NP-Likeness -1.03

Activity Summary

IC50 2 meas. best 8.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL231
IC50 8.18 8.18 6.6 1
Substance-P receptor
CHEMBL3942
IC50 8.18 8.18 6.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor IC50 = 6.54 nM 8.18 Antagonistic activity against Tachykinin receptor 1 -
Histamine H1 receptor IC50 = 6.6 nM 8.18 Antagonistic activity against histamine H1 receptor -

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