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Compound Detail

CHEMBL2334881

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COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCCO4

Basic Information

ChEMBL ID CHEMBL2334881
Phase Preclinical
Structure Type MOL
InChI Key XTOFAUDOQPKYRI-INIZCTEOSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

339.4
MW (Da)
2.83
ALogP
5
HBA
1
HBD
51.2
PSA (Ų)
0.87
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H21NO4
MW 339.39
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness 1.11

Activity Summary

Ki 3 meas. best 8.12
IC50 1 meas. best 7.83

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(1A) dopamine receptor
CHEMBL2056
Ki 8.12 8.12 7.5 1
D(1A) dopamine receptor
CHEMBL2056
IC50 7.83 7.83 14.7 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 6.68 6.68 208.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 6.44 6.44 363.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23332346 10.1016/j.bmc.2012.12.016 5-hydroxytryptamine receptor 1A 2
23332346 10.1016/j.bmc.2012.12.016 5-hydroxytryptamine receptor 2A 2
23332346 10.1016/j.bmc.2012.12.016 D(2) dopamine receptor 2
23332346 10.1016/j.bmc.2012.12.016 D(1A) dopamine receptor 2

Data from ChEMBL 36 via Core Engine