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Compound Detail

CHEMBL1795628

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COc1ccccc1C(=O)c1cnc(NC2CCN(C(=O)Nc3ccccc3)CC2)nc1N

Basic Information

ChEMBL ID CHEMBL1795628
Phase Preclinical
Structure Type MOL
InChI Key XBQHFXCPZMGKKQ-UHFFFAOYSA-N
4
Targets
7
Activities
1
Assay Types
1
PK Parameters
9
Publications
0
Known Names

Molecular Properties

446.5
MW (Da)
3.41
ALogP
7
HBA
3
HBD
122.5
PSA (Ų)
0.50
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 C24H26N6O3
MW 446.51
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.45

Activity Summary

IC50 7 meas. best 7.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei brucei
CHEMBL612851
IC50 7.35 7.2233 45.0 3
Trypanosoma brucei
CHEMBL612849
IC50 7.16 7.16 70.0 1
Leishmania donovani
CHEMBL367
IC50 6.0 6.0 1000.0 2
L929
CHEMBL612267
IC50 5.12 5.12 7500.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 1.6 hr -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21507639 10.1016/j.bmcl.2011.03.097 MDCK 4
21507639 10.1016/j.bmcl.2011.03.097 Trypanosoma brucei brucei 3
23063403 10.1016/j.bmcl.2012.09.044 Leishmania donovani 2
23063403 10.1016/j.bmcl.2012.09.044 Trypanosoma brucei brucei 2
21507639 10.1016/j.bmcl.2011.03.097 L929 1
21507639 10.1016/j.bmcl.2011.03.097 ADMET 1
21507639 10.1016/j.bmcl.2011.03.097 No relevant target 1
23063403 10.1016/j.bmcl.2012.09.044 Trypanosoma brucei 1
25072876 10.1016/j.ejmech.2014.07.092 Trypanosoma brucei 1

Data from ChEMBL 36 via Core Engine