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Compound Detail

CHEMBL325645

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CO/N=C/c1ccc(OCCCc2c[nH]cn2)cc1.O=C(O)/C=C\C(=O)O

Basic Information

ChEMBL ID CHEMBL325645
Phase Preclinical
Structure Type MOL
InChI Key IUFPANKLVNADJQ-DZJWKFROSA-N
Parent Compound CHEMBL1183956
Active Moiety CHEMBL1183956
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

259.3
MW (Da)
2.40
ALogP
4
HBA
1
HBD
59.5
PSA (Ų)
0.47
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 C18H21N3O6
MW 375.38
Aromatic Rings 2
Heavy Atoms 19
NP-Likeness -0.86

Activity Summary

Ki 2 meas. best 7.9
Kd 1 meas. best 7.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL4124
Ki 7.9 7.895 12.6 2
Cavia porcellus
CHEMBL369
Kd 7.3 7.3 50.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10966752 10.1021/jm000971p Histamine H3 receptor 2
10966752 10.1021/jm000971p Mus musculus 1
10966752 10.1021/jm000971p Cavia porcellus 1
10966752 10.1021/jm000971p Histamine H2 receptor 1
10966752 10.1021/jm000971p Histamine H1 receptor 1

Data from ChEMBL 36 via Core Engine