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Compound Detail

CHEMBL1795632

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COc1ccccc1C(=O)c1cnc(NC2CCN(c3nccs3)CC2)nc1N

Basic Information

ChEMBL ID CHEMBL1795632
Phase Preclinical
Structure Type MOL
InChI Key AWBJJDIBNKVTHU-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

410.5
MW (Da)
2.84
ALogP
9
HBA
2
HBD
106.3
PSA (Ų)
0.60
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H22N6O2S
MW 410.50
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.70

Activity Summary

IC50 1 meas. best 5.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei brucei
CHEMBL612851
IC50 5.51 5.51 3100.0 1

Pharmacokinetic Data

Parameter Value Units Species
t1/2 - - -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypanosoma brucei brucei IC50 = 3100.0 nM 5.51 Antitrypanosomal activity against Trypanosoma brucei brucei 21507639

Literature References

PubMed DOI Target Context # Activities
21507639 10.1016/j.bmcl.2011.03.097 Trypanosoma brucei brucei 1
21507639 10.1016/j.bmcl.2011.03.097 L929 1
21507639 10.1016/j.bmcl.2011.03.097 No relevant target 1
21507639 10.1016/j.bmcl.2011.03.097 ADMET 1

Data from ChEMBL 36 via Core Engine