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Compound Detail

CHEMBL1357558

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CSc1ccc2c(c1)N(CC[C@H]1CCCCN1C)c1ccccc1S2

Basic Information

ChEMBL ID CHEMBL1357558
Phase Preclinical
Structure Type MOL
InChI Key KLBQZWRITKRQQV-MRXNPFEDSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

370.6
MW (Da)
5.89
ALogP
4
HBA
0
HBD
6.5
PSA (Ų)
0.62
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C21H26N2S2
MW 370.59
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -1.03

Activity Summary

IC50 2 meas. best 5.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase pim-1
CHEMBL2147
IC50 5.15 5.15 7030.0 1
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 4.78 4.78 16570.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine/threonine-protein kinase pim-1 IC50 = 7030.0 nM 5.15 Inhibition of PIM-1 (unknown origin) after 1 hr by HTRF assay -
Trypanosoma brucei rhodesiense IC50 = 16570.0 nM 4.78 DNDI: HAT in Vitro, 72 hour -

Literature References

PubMed DOI Target Context # Activities
28671460 10.1021/acs.jmedchem.7b00285 Myeloperoxidase 4
- 10.6019/CHEMBL3392926 Leishmania donovani 2
- 10.6019/CHEMBL3392926 NON-PROTEIN TARGET 2
- 10.1039/C4MD00030G Serine/threonine-protein kinase pim-1 1
- 10.6019/CHEMBL3392926 Trypanosoma cruzi 1
- 10.6019/CHEMBL3392926 Trypanosoma brucei rhodesiense 1

Data from ChEMBL 36 via Core Engine