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Compound Detail

CHEMBL485207

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Br.Oc1cc2c(c(-c3ccc4ccccc4c3)c1O)CCNCC2c1ccccc1

Basic Information

ChEMBL ID CHEMBL485207
Phase Preclinical
Structure Type MOL
InChI Key HPGVTZSRTOLFTD-UHFFFAOYSA-N
Parent Compound CHEMBL1186978
Active Moiety CHEMBL1186978
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

381.5
MW (Da)
5.20
ALogP
3
HBA
3
HBD
52.5
PSA (Ų)
0.42
QED
1
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H24BrNO2
MW 462.39
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness 0.62

Activity Summary

Ki 3 meas. best 7.25

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(1A) dopamine receptor
CHEMBL2056
Ki 7.25 7.25 56.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 6.43 6.43 375.0 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 5.96 5.96 1083.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18835172 10.1016/j.bmc.2008.09.049 D(1A) dopamine receptor 1
18835172 10.1016/j.bmc.2008.09.049 D(2) dopamine receptor 1
18835172 10.1016/j.bmc.2008.09.049 5-hydroxytryptamine receptor 1A 1
18835172 10.1016/j.bmc.2008.09.049 5-hydroxytryptamine receptor 2A 1

Data from ChEMBL 36 via Core Engine