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Compound Detail

CHEMBL330462

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CCOc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(OC)c(OC)c3)C2)cc(OCC)c1OCC

Basic Information

ChEMBL ID CHEMBL330462
Phase Preclinical
Structure Type MOL
InChI Key GMDILGHWZUFMEQ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

807.0
MW (Da)
8.21
ALogP
10
HBA
0
HBD
104.6
PSA (Ų)
0.09
QED
2
Ro5 Violations
17
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C47H55FN4O7
MW 806.98
Aromatic Rings 5
Heavy Atoms 59
NP-Likeness -0.90

Activity Summary

IC50 2 meas. best 8.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL3942
IC50 8.23 8.23 5.9 1
Histamine H1 receptor
CHEMBL231
IC50 8.17 8.17 6.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor IC50 = 5.91 nM 8.23 Antagonistic activity against Tachykinin receptor 1 -
Histamine H1 receptor IC50 = 6.8 nM 8.17 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