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Compound Detail

CHEMBL5219240

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CN1CCN(c2nc(N)nc(C(C)(C)Sc3ccc4ccccc4c3)n2)CC1

Basic Information

ChEMBL ID CHEMBL5219240
Phase Preclinical
Structure Type MOL
InChI Key AFNNYMZEMGROFW-UHFFFAOYSA-N
5
Targets
6
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

394.6
MW (Da)
3.39
ALogP
7
HBA
1
HBD
71.2
PSA (Ų)
0.68
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H26N6S
MW 394.55
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.07

Activity Summary

Ki 6 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 7.96 7.96 11.0 2
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 7.41 7.41 39.0 1
D(2) dopamine receptor
CHEMBL217
Ki 6.52 6.52 300.0 1
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 6.21 6.21 610.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 5.64 5.64 2290.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35981459 10.1016/j.ejmech.2022.114645 5-hydroxytryptamine receptor 6 2
35981459 10.1016/j.ejmech.2022.114645 5-hydroxytryptamine receptor 1A 1
35981459 10.1016/j.ejmech.2022.114645 5-hydroxytryptamine receptor 2A 1
35981459 10.1016/j.ejmech.2022.114645 5-hydroxytryptamine receptor 7 1
35981459 10.1016/j.ejmech.2022.114645 D(2) dopamine receptor 1
38190615 10.1021/acs.jmedchem.3c02148 5-hydroxytryptamine receptor 6 1

Data from ChEMBL 36 via Core Engine