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Compound Detail

CHEMBL3325607

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CNC(=O)c1ccc(-c2cnc3cnc(C(=O)N(C)c4ccc(C#N)cc4)cn23)cc1

Basic Information

ChEMBL ID CHEMBL3325607
Phase Preclinical
Structure Type MOL
InChI Key SVIYAQDUUGCJJB-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
8
PK Parameters
8
Publications
0
Known Names

Molecular Properties

410.4
MW (Da)
2.90
ALogP
6
HBA
1
HBD
103.4
PSA (Ų)
0.56
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H18N6O2
MW 410.44
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.68

Activity Summary

IC50 4 meas. best 7.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium cynomolgi
CHEMBL613883
IC50 7.09 7.06 81.0 2
Plasmodium falciparum
CHEMBL364
IC50 6.88 6.88 131.0 1
Plasmodium yoelii
CHEMBL612889
IC50 6.54 6.54 290.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 5089.46 ng.hr.mL-1 Mus musculus
CL 34.0 mL.min-1.kg-1 Mus musculus
Cmax 5200.0 nM Mus musculus
F 51.9 % Mus musculus
T1/2 2.083 hr Mus musculus
T1/2 1.63 hr Mus musculus
T1/2 0.42 hr Mus musculus
Tmax 0.5 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25147620 10.1021/ml500244m Mus musculus 8
25147620 10.1021/ml500244m Plasmodium cynomolgi 2
25147620 10.1021/ml500244m No relevant target 1
25147620 10.1021/ml500244m Plasmodium yoelii 1
25147620 10.1021/ml500244m Plasmodium falciparum 1
25147620 10.1021/ml500244m ADMET 1
25147620 10.1021/ml500244m Liver 1
25147620 10.1021/ml500244m Plasmodium berghei 1

Data from ChEMBL 36 via Core Engine