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Compound Detail

CHEMBL36517

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O=c1oc2cc(CN3CCN(Cc4ccc(Cl)cc4)CC3)ccc2c(O)c1[N+](=O)[O-]

Basic Information

ChEMBL ID CHEMBL36517
Phase Preclinical
Structure Type MOL
InChI Key LCBFIEXOJLHCMZ-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

429.9
MW (Da)
3.38
ALogP
7
HBA
1
HBD
100.1
PSA (Ų)
0.38
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H20ClN3O5
MW 429.86
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.79

Activity Summary

IC50 2 meas. best 4.85
Kd 1 meas. best 5.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL3943
Kd 5.6 5.6 2511.9 1
Rattus norvegicus
CHEMBL376
IC50 4.85 4.465 14000.0 2

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