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Compound Detail

CHEMBL312082

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CC(C#Cc1ccc(CN2CCN([C@H](c3ccccc3)c3ccc(Cl)cc3)CC2)o1)N(O)C(N)=O

Basic Information

ChEMBL ID CHEMBL312082
Phase Preclinical
Structure Type MOL
InChI Key FJXRDARXFNFHEP-NBXNUCLWSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

493.0
MW (Da)
4.35
ALogP
5
HBA
2
HBD
86.2
PSA (Ų)
0.30
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H29ClN4O3
MW 493.01
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.79

Activity Summary

IC50 1 meas. best 5.46
Ki 1 meas. best 6.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL231
Ki 6.72 6.72 190.0 1
Polyunsaturated fatty acid 5-lipoxygenase
CHEMBL215
IC50 5.46 5.46 3500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

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

Data from ChEMBL 36 via Core Engine