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Compound Detail

CHEMBL1836719

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CSc1ccc(-c2cc3ncnc(SCC(=O)O)c3s2)cc1

Basic Information

ChEMBL ID CHEMBL1836719
Phase Preclinical
Structure Type MOL
InChI Key KJCQGDBVLKOAHP-UHFFFAOYSA-N
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

348.5
MW (Da)
4.26
ALogP
6
HBA
1
HBD
63.1
PSA (Ų)
0.55
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H12N2O2S3
MW 348.47
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -1.66

Activity Summary

IC50 3 meas. best 7.7
Kd 2 meas. best 8.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase 17B
CHEMBL3980
Kd 8.42 8.42 3.8 1
Serine/threonine-protein kinase 17B
CHEMBL3980
IC50 7.7 7.19 20.0 2
Serine/threonine-protein kinase 17A
CHEMBL4525
Kd 6.64 6.64 230.0 1
Mitogen-activated protein kinase kinase kinase 8
CHEMBL4899
IC50 4.47 4.47 34000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33215924 10.1021/acs.jmedchem.0c01174 Serine/threonine-protein kinase 17B 5
33215924 10.1021/acs.jmedchem.0c01174 Serine/threonine-protein kinase 17A 2
21862328 10.1016/j.bmcl.2011.07.069 Mitogen-activated protein kinase kinase kinase 8 1
33215924 10.1021/acs.jmedchem.0c01174 Unchecked 1
33215924 10.1021/acs.jmedchem.0c01174 ADMET 1
33215924 10.1021/acs.jmedchem.0c01174 No relevant target 1
- 10.6019/CHEMBL5724564 Hepatocyte spheroids 1

Data from ChEMBL 36 via Core Engine