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Compound Detail

CHEMBL423786

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C[C@@H](NC(=O)c1cccs1)C(=O)N1CCN(CCCOc2ccc(-c3noc(-c4ccccc4)n3)c(F)c2)CC1

Basic Information

ChEMBL ID CHEMBL423786
Phase Preclinical
Structure Type MOL
InChI Key IXXJRACDUQTBHS-HXUWFJFHSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

563.7
MW (Da)
4.34
ALogP
8
HBA
1
HBD
100.8
PSA (Ų)
0.29
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H30FN5O4S
MW 563.66
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -2.09

Activity Summary

Ki 2 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL4124
Ki 8.3 8.3 5.0 1
Histamine H3 receptor
CHEMBL264
Ki 7.4 7.4 40.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14741266 10.1016/j.bmcl.2003.11.038 Histamine H3 receptor 2

Data from ChEMBL 36 via Core Engine