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Compound Detail

CHEMBL4536315

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COc1ccc2[nH]c(C)c(CCNCc3ccc(-c4ccc(O)cc4)o3)c2c1

Basic Information

ChEMBL ID CHEMBL4536315
Phase Preclinical
Structure Type MOL
InChI Key YVYFBBDHUFSWDX-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

376.5
MW (Da)
4.78
ALogP
4
HBA
3
HBD
70.4
PSA (Ų)
0.41
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H24N2O3
MW 376.46
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -0.59

Activity Summary

Ki 4 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 7.68 7.68 21.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 7.38 7.38 42.0 1
D(2) dopamine receptor
CHEMBL217
Ki 6.78 6.78 167.0 1
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 5.27 5.27 5316.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 183.6 mL.min-1.g-1 Rattus norvegicus
T1/2 0.1333 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31734022 10.1016/j.ejmech.2019.111857 ADMET 2
31734022 10.1016/j.ejmech.2019.111857 5-hydroxytryptamine receptor 6 1
31734022 10.1016/j.ejmech.2019.111857 5-hydroxytryptamine receptor 2A 1
31734022 10.1016/j.ejmech.2019.111857 5-hydroxytryptamine receptor 7 1
31734022 10.1016/j.ejmech.2019.111857 D(2) dopamine receptor 1

Data from ChEMBL 36 via Core Engine