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Compound Detail

CHEMBL3430999

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O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCCCC1c1cccnc1

Basic Information

ChEMBL ID CHEMBL3430999
Phase Preclinical
Structure Type MOL
InChI Key QKORLSWPVRPZBR-UHFFFAOYSA-N
7
Targets
14
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

339.8
MW (Da)
4.58
ALogP
2
HBA
1
HBD
49.0
PSA (Ų)
0.74
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C19H18ClN3O
MW 339.83
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.46

Activity Summary

IC50 14 meas. best 7.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sterol 14-alpha demethylase
CHEMBL1075110
IC50 7.2 7.2 63.1 1
Trypanosoma cruzi
CHEMBL368
IC50 6.9 6.225 125.9 4
Leishmania donovani
CHEMBL367
IC50 5.0 4.65 10000.0 4
Trypanosoma brucei brucei
CHEMBL612851
IC50 4.8 4.7 15848.9 2
NAD-dependent protein deacetylase
CHEMBL4523517
IC50 4.74 4.74 18200.0 1
HepG2
CHEMBL395
IC50 4.4 4.4 39810.7 1
NIH3T3
CHEMBL614822
IC50 4.4 4.4 39810.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sterol 14-alpha demethylase IC50 = 63.1 nM 7.2 GSK_TCAKS: pIC50 CYP51 from Trypanosoma cruzi. -
Trypanosoma cruzi IC50 = 125.89 nM 6.9 GSK_TCAKS: pIC50 Trypanosoma cruzi Imaging: Infected Cells. H9c2 cells were seed... -
Trypanosoma cruzi IC50 = 125.89 nM 6.9 GSK_TCAKS: pIC50 Trypanosoma cruzi Imaging: Amastigotes/Cell. H9c2 cells were se... -
Trypanosoma cruzi IC50 = 251.19 nM 6.6 GSK_TCAKS: pIC50 Trypanosoma cruzi viability assay using beta-GAL activity. This... -
Leishmania donovani IC50 = 10000.0 nM 5.0 GSK_TCAKS: pIC50 Leishmania donovani Imaging: Amastigotes/Macrophages. Assay pla... -
Leishmania donovani IC50 = 15848.93 nM 4.8 GSK_TCAKS: pIC50 Leishmania donovani Imaging: THP-1 Host Macrophages. Assay plat... -
Trypanosoma brucei brucei IC50 = 15848.93 nM 4.8 GSK_TCAKS: pIC50 Trypanosoma brucei viability assay using luminiscence. Assay pl... -
NAD-dependent protein deacetylase IC50 = 18200.0 nM 4.74 Inhibition of recombinant Schistosoma mansoni sirtuin 2 (21 to 322 residues) exp... 31496251
Trypanosoma brucei brucei IC50 = 25118.86 nM 4.6 GSK_TCAKS: pIC50 Trypanosoma brucei viability assay using fluorescence intensity... -
Trypanosoma cruzi IC50 = 31622.78 nM 4.5 GSK_TCAKS: pIC50 H2C9 Imaging: H9c2 Host Cardiomyocytes. H9c2 cells were seeded ... -
Leishmania donovani IC50 = 31622.78 nM 4.5 GSK_TCAKS: pIC50 Leishmania donovani Imaging: Infected Macrophages. Assay plates... -
HepG2 IC50 = 39810.72 nM 4.4 GSK_TCAKS: pIC50 HepG2 human cell line viability assay using luminiscence. Activ... -
NIH3T3 IC50 = 39810.72 nM 4.4 GSK_TCAKS: pIC50 NIH 3T3 cell line viability assay using luminiscence. Tissue cu... -
Leishmania donovani IC50 = 50118.72 nM 4.3 GSK_TCAKS: pIC50 Leishmania donovani viability assay using fluorescence intensit... -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3430912 Trypanosoma cruzi 4
- 10.6019/CHEMBL3430912 Leishmania donovani 4
- 10.6019/CHEMBL3430912 Trypanosoma brucei brucei 2
- 10.6019/CHEMBL3430912 HepG2 1
- 10.6019/CHEMBL3430912 NIH3T3 1
- 10.6019/CHEMBL3430912 Sterol 14-alpha demethylase 1
31496251 10.1021/acs.jmedchem.9b00638 NAD-dependent protein deacetylase 1
31496251 10.1021/acs.jmedchem.9b00638 NAD-dependent protein deacetylase sirtuin-2 1

Data from ChEMBL 36 via Core Engine