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Compound Detail

CHEMBL4780452

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COc1ccc(-c2ccccc2N2CCN(C[C@@H](O)COc3cnccn3)CC2)cc1

Basic Information

ChEMBL ID CHEMBL4780452
Phase Preclinical
Structure Type MOL
InChI Key ATGGHACHMARXLW-HXUWFJFHSA-N
2
Targets
2
Activities
1
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

420.5
MW (Da)
2.71
ALogP
7
HBA
1
HBD
71.0
PSA (Ų)
0.60
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H28N4O3
MW 420.51
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.10

Activity Summary

Ki 2 meas. best 7.79

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 7.79 7.79 16.1 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 7.08 7.08 82.9 1

Pharmacokinetic Data

Parameter Value Units Species
CL 23.1 mL.min-1.g-1 Rattus norvegicus
T1/2 0.5 hr Rattus norvegicus
T1/2 2.217 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32442850 10.1016/j.ejmech.2020.112395 ADMET 4
32442850 10.1016/j.ejmech.2020.112395 5-hydroxytryptamine receptor 7 1
32442850 10.1016/j.ejmech.2020.112395 5-hydroxytryptamine receptor 1A 1
32442850 10.1016/j.ejmech.2020.112395 Albumin 1

Data from ChEMBL 36 via Core Engine