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Compound Detail

CHEMBL420934

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Cc1c(OCCCN2CCN(Cc3cccc(Cl)c3)CC2)ccc2c(O)c3nnnc-3oc12

Basic Information

ChEMBL ID CHEMBL420934
Phase Preclinical
Structure Type MOL
InChI Key ZVVPUTHIHTUDJY-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

468.0
MW (Da)
3.98
ALogP
8
HBA
1
HBD
87.8
PSA (Ų)
0.41
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 C24H26ClN5O3
MW 467.96
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.21

Activity Summary

IC50 1 meas. best 6.0
Kd 1 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL3943
Kd 8.4 8.4 4.0 1
Rattus norvegicus
CHEMBL376
IC50 6.0 6.0 1000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2431143 10.1021/jm00161a022 Rattus norvegicus 2
2431143 10.1021/jm00161a022 Histamine H1 receptor 1

Data from ChEMBL 36 via Core Engine