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Compound Detail

CHEMBL4105102

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Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4scnc34)CC1)CCCC2O

Basic Information

ChEMBL ID CHEMBL4105102
Phase Preclinical
Structure Type MOL
InChI Key ORRGIUCJVXIACQ-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

425.6
MW (Da)
2.35
ALogP
8
HBA
1
HBD
74.5
PSA (Ų)
0.69
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H27N5O2S
MW 425.56
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.90

Activity Summary

EC50 1 meas. best 7.16
IC50 1 meas. best 5.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL214
EC50 7.16 7.16 69.7 1
5-hydroxytryptamine receptor 2A
CHEMBL224
IC50 5.64 5.64 2300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28774576 10.1016/j.bmc.2017.07.040 5-hydroxytryptamine receptor 1A 1
28774576 10.1016/j.bmc.2017.07.040 D(2) dopamine receptor 1
28774576 10.1016/j.bmc.2017.07.040 5-hydroxytryptamine receptor 2A 1

Data from ChEMBL 36 via Core Engine