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Compound Detail

CHEMBL4871408

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CN1C(=S)[C@@H](NC(=O)c2n[nH]c(Cc3ccccc3)n2)COc2ccccc21

Basic Information

ChEMBL ID CHEMBL4871408
Phase Preclinical
Structure Type MOL
InChI Key IECXSYCNRXFRJS-AWEZNQCLSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

393.5
MW (Da)
2.35
ALogP
5
HBA
2
HBD
83.1
PSA (Ų)
0.66
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H19N5O2S
MW 393.47
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.97

Activity Summary

EC50 2 meas. best 8.55
Kd 1 meas. best 7.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HT-29
CHEMBL384
EC50 8.55 8.55 2.8 2
Receptor-interacting serine/threonine-protein kinase 1
CHEMBL5464
Kd 7.51 7.51 31.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33930803 10.1016/j.ejmech.2021.113484 HT-29 3
33930803 10.1016/j.ejmech.2021.113484 Receptor-interacting serine/threonine-protein kinase 1 3
33930803 10.1016/j.ejmech.2021.113484 Receptor-interacting serine/threonine-protein kinase 3 3
33930803 10.1016/j.ejmech.2021.113484 Mixed lineage kinase domain-like protein 2
36724216 10.1021/acs.jmedchem.2c02067 HT-29 2
35398729 10.1016/j.ejmech.2022.114345 HT-29 1
35398729 10.1016/j.ejmech.2022.114345 Receptor-interacting serine/threonine-protein kinase 1 1

Data from ChEMBL 36 via Core Engine