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Compound Detail

CHEMBL5209381

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COc1ccccc1N1CCN(CCN2CCN(C(=O)c3nn(C)c4ccccc34)CC2)CC1

Basic Information

ChEMBL ID CHEMBL5209381
Phase Preclinical
Structure Type MOL
InChI Key UDFSBKOWQSCWPJ-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

462.6
MW (Da)
2.16
ALogP
7
HBA
0
HBD
57.1
PSA (Ų)
0.56
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H34N6O2
MW 462.60
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.47

Activity Summary

IC50 2 meas. best 5.52
Ki 2 meas. best 6.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(2) dopamine receptor
CHEMBL217
Ki 6.2 6.2 630.0 1
5-hydroxytryptamine receptor 3A
CHEMBL3666
IC50 5.52 5.52 3000.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 5.08 5.08 8300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35176563 10.1016/j.ejmech.2022.114193 D(2) dopamine receptor 1
35176563 10.1016/j.ejmech.2022.114193 5-hydroxytryptamine receptor 2A 1
35176563 10.1016/j.ejmech.2022.114193 5-hydroxytryptamine receptor 3A 1
35176563 10.1016/j.ejmech.2022.114193 CHO-K1 1
35176563 10.1016/j.ejmech.2022.114193 ADMET 1

Data from ChEMBL 36 via Core Engine