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Compound Detail

CHEMBL4482871

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Cl.Cl.Cl.N=C(NCCCCN1CCN(CCCCCCCOc2ccccc2)CC1)NCc1ccccc1

Basic Information

ChEMBL ID CHEMBL4482871
Phase Preclinical
Structure Type MOL
InChI Key GEDAFFSBLGCUJQ-UHFFFAOYSA-N
Parent Compound CHEMBL4595050
Active Moiety CHEMBL4595050
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

479.7
MW (Da)
4.73
ALogP
4
HBA
3
HBD
63.6
PSA (Ų)
0.18
QED
0
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H48Cl3N5O
MW 589.10
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.62

Activity Summary

Kd 2 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL5076
Kd 8.1 8.1 7.9 1
Histamine H1 receptor
CHEMBL3943
Kd 7.1 7.1 79.4 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30881612 10.1039/C8MD00527C Histamine H1 receptor 1
30881612 10.1039/C8MD00527C Histamine H3 receptor 1

Data from ChEMBL 36 via Core Engine