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Compound Detail

CHEMBL1795629

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COc1ccccc1C(=O)c1cnc(NC2CCN(c3nc4ccccc4[nH]3)CC2)nc1N

Basic Information

ChEMBL ID CHEMBL1795629
Phase Preclinical
Structure Type MOL
InChI Key ABTBBCOJRBCDEH-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

443.5
MW (Da)
3.26
ALogP
8
HBA
3
HBD
122.0
PSA (Ų)
0.39
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 C24H25N7O2
MW 443.51
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.32

Activity Summary

IC50 2 meas. best 7.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei brucei
CHEMBL612851
IC50 7.06 7.06 88.0 1
L929
CHEMBL612267
IC50 5.12 5.12 7600.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 1.6 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypanosoma brucei brucei IC50 = 88.0 nM 7.06 Antitrypanosomal activity against Trypanosoma brucei brucei 21507639
L929 IC50 = 7600.0 nM 5.12 Cytotoxicity against mouse L929 cells 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