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Compound Detail

CHEMBL484538

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Br.Cc1cccc(-c2c(O)c(O)cc3c2CCN(C)CC3c2cccc(C)c2)c1

Basic Information

ChEMBL ID CHEMBL484538
Phase Preclinical
Structure Type MOL
InChI Key WKXBRVOJFDBSLP-UHFFFAOYSA-N
Parent Compound CHEMBL1186967
Active Moiety CHEMBL1186967
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

373.5
MW (Da)
5.00
ALogP
3
HBA
2
HBD
43.7
PSA (Ų)
0.62
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 C25H28BrNO2
MW 454.41
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness 0.24

Activity Summary

Ki 3 meas. best 8.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(1A) dopamine receptor
CHEMBL2056
Ki 8.17 8.17 6.8 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 6.92 6.92 121.0 1
D(2) dopamine receptor
CHEMBL217
Ki 6.68 6.68 210.0 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