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Compound Detail

CHEMBL416357

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CCCN1CCCN(c2nc3ccccc3n2CCOCC)CC1

Basic Information

ChEMBL ID CHEMBL416357
Phase Preclinical
Structure Type MOL
InChI Key FYCVRXDLYQVHNU-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

330.5
MW (Da)
2.99
ALogP
5
HBA
0
HBD
33.5
PSA (Ų)
0.73
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 C19H30N4O
MW 330.48
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -2.04

Activity Summary

IC50 1 meas. best 8.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL3943
IC50 8.08 8.08 8.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histamine H1 receptor IC50 = 8.4 nM 8.08 In vitro inhibition of histamine-induced contractions in guinea pig ileum 2879912

Literature References

PubMed DOI Target Context # Activities
2879912 10.1021/jm00157a010 Histamine H1 receptor 1
2879912 10.1021/jm00157a010 Unchecked 1

Data from ChEMBL 36 via Core Engine