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Compound Detail

CHEMBL467047

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Cc1nc(N)c2ncn([C@@H]3O[C@H](CN(C)C/C=C\CN)[C@@H](O)[C@H]3O)c2n1

Basic Information

ChEMBL ID CHEMBL467047
Phase Preclinical
Structure Type MOL
InChI Key MTDBNJKMVASAKC-LNNUBQDUSA-N
1
Targets
1
Activities
1
Assay Types
17
PK Parameters
19
Publications
0
Known Names

Molecular Properties

363.4
MW (Da)
-1.22
ALogP
10
HBA
4
HBD
148.6
PSA (Ų)
0.46
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 C16H25N7O3
MW 363.42
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness 0.32

Activity Summary

IC50 1 meas. best 10.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 10.0 10.0 0.1 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 17920.0 ng.hr.mL-1 Mus musculus
AUC 1300.0 ng.hr.mL-1 Mus musculus
AUC 49.0 ng.hr.mL-1 Rattus norvegicus
AUC 681.0 ng.hr.mL-1 Rattus norvegicus
CL 81.0 mL.min-1.kg-1 Rattus norvegicus
CL 11.0 mL.min-1.kg-1 Rattus norvegicus
CL 11.0 mL.min-1.kg-1 Rattus norvegicus
CL 4.2 mL.min-1.kg-1 Homo sapiens
CL 4.2 mL.min-1.kg-1 Homo sapiens
Cmax 101535.41 nM Mus musculus
Cmax 1816.08 nM Mus musculus
Cmax 107.31 nM Rattus norvegicus
F 2.1 % Rattus norvegicus
T1/2 7.43 hr Mus musculus
T1/2 1.53 hr Rattus norvegicus
T1/2 3.17 hr Rattus norvegicus
Tmax 0.25 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19289530 10.1128/aac.01674-08 Rattus norvegicus 9
19289530 10.1128/aac.01674-08 Trypanosoma brucei brucei 6
19289530 10.1128/aac.01674-08 Blood 2
19289530 10.1128/aac.01674-08 Brain 2
19289530 10.1128/aac.01674-08 ADMET 2
19289530 10.1128/aac.01674-08 S-adenosylmethionine decarboxylase proenzyme 2
19289530 10.1128/aac.01674-08 Plasma 2
19289530 10.1128/aac.01674-08 Liver microsomes 2
19289530 10.1128/aac.01674-08 Hepatocyte 2
19289530 10.1128/aac.01674-08 Cytochrome P450 1A2 1
19419862 10.1016/j.bmcl.2009.04.096 Trypanosoma brucei rhodesiense 1
19289530 10.1128/aac.01674-08 Cytochrome P450 2C19 1
19289530 10.1128/aac.01674-08 Cytochrome P450 2C9 1
19289530 10.1128/aac.01674-08 Cytochrome P450 2D6 1
19289530 10.1128/aac.01674-08 Cytochrome P450 3A4 1
19289530 10.1128/aac.01674-08 No relevant target 1
19289530 10.1128/aac.01674-08 Trypanosoma brucei rhodesiense 1
19289530 10.1128/aac.01674-08 Mus musculus 1
19419862 10.1016/j.bmcl.2009.04.096 Trypanosoma brucei brucei 1

Data from ChEMBL 36 via Core Engine