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Compound Detail

CHEMBL73706

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NC(=O)N(O)CCC#Cc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)o1

Basic Information

ChEMBL ID CHEMBL73706
Phase Preclinical
Structure Type MOL
InChI Key CJHFYNOETGOKCU-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

494.5
MW (Da)
3.98
ALogP
5
HBA
2
HBD
86.2
PSA (Ų)
0.29
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H28F2N4O3
MW 494.54
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.88

Activity Summary

IC50 1 meas. best 6.77
Ki 1 meas. best 6.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Polyunsaturated fatty acid 5-lipoxygenase
CHEMBL215
IC50 6.77 6.77 170.0 1
Histamine H1 receptor
CHEMBL231
Ki 6.26 6.26 550.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15081022 10.1016/j.bmcl.2004.02.005 Polyunsaturated fatty acid 5-lipoxygenase 2
15081022 10.1016/j.bmcl.2004.02.005 Histamine H1 receptor 1

Data from ChEMBL 36 via Core Engine