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Compound Detail

CHEMBL304223

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O=C(O)/C=C/C(=O)O.O=C(O)c1ccc2c(c1)/C(=C\CCN1CCCC1)c1ccccc1CO2

Basic Information

ChEMBL ID CHEMBL304223
Phase Preclinical
Structure Type MOL
InChI Key LPGJTHLMKVNKCM-DRGVERFISA-N
Parent Compound CHEMBL1183550
Active Moiety CHEMBL1183550
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

349.4
MW (Da)
4.19
ALogP
3
HBA
1
HBD
49.8
PSA (Ų)
0.90
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H27NO7
MW 465.50
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.16

Activity Summary

Ki 1 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H1 receptor
CHEMBL3943
Ki 8.3 8.3 5.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
1350797 10.1021/jm00089a020 Rattus norvegicus 1
1350797 10.1021/jm00089a020 Cavia porcellus 1
1350797 10.1021/jm00089a020 Histamine H1 receptor 1
1350797 10.1021/jm00089a020 Muscarinic acetylcholine receptor M1 1

Data from ChEMBL 36 via Core Engine