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Compound Detail

CHEMBL286094

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O=c1oc2cc(OCCN3CCN(Cc4ccc(Cl)cc4)CC3)ccc2c(O)c1[N+](=O)[O-]

Basic Information

ChEMBL ID CHEMBL286094
Phase Preclinical
Structure Type MOL
InChI Key IUNOGVIXKGNTSQ-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

459.9
MW (Da)
3.26
ALogP
8
HBA
1
HBD
109.3
PSA (Ų)
0.33
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 C22H22ClN3O6
MW 459.89
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.97

Activity Summary

IC50 2 meas. best 4.0
Kd 1 meas. best 6.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL3943
Kd 6.8 6.8 158.5 1
Rattus norvegicus
CHEMBL376
IC50 4.0 4.0 100000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
6208360 10.1021/jm00377a013 Rattus norvegicus 2
6208360 10.1021/jm00377a013 Histamine H1 receptor 1

Data from ChEMBL 36 via Core Engine