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Compound Detail

CHEMBL4646408

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Nc1ncnc2c1c(Oc1cc(C(F)(F)F)ccn1)nn2[C@@H]1CCCC[C@H]1O

Basic Information

ChEMBL ID CHEMBL4646408
Phase Preclinical
Structure Type MOL
InChI Key QBGXAQUTKHIMNE-GHMZBOCLSA-N
7
Targets
9
Activities
2
Assay Types
9
PK Parameters
19
Publications
0
Known Names

Molecular Properties

394.4
MW (Da)
3.09
ALogP
8
HBA
2
HBD
112.0
PSA (Ų)
0.70
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H17F3N6O2
MW 394.36
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.66

Activity Summary

EC50 8 meas. best 7.11
IC50 1 meas. best 8.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 8.18 8.18 6.6 1
Toxoplasma gondii
CHEMBL612888
EC50 7.11 6.9333 77.0 3
Cytochrome P450 2D6
CHEMBL289
EC50 4.3 4.3 50000.0 1
Cytochrome P450 1A2
CHEMBL3356
EC50 4.3 4.3 50000.0 1
Cytochrome P450 2C9
CHEMBL3397
EC50 4.3 4.3 50000.0 1
Cytochrome P450 3A4
CHEMBL340
EC50 4.3 4.3 50000.0 1
Cytochrome P450 2C19
CHEMBL3622
EC50 4.3 4.3 50000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1100.0 ng.hr.mL-1 Mus musculus
CL 8.6 mL.min-1.kg-1 Homo sapiens
Cmax 1572.17 nM Mus musculus
F 48.9 % Mus musculus
Fu 0.243 - Mus musculus
Fu 0.041 - Mus musculus
T1/2 1.1 hr Mus musculus
T1/2 2.417 hr Homo sapiens
T1/2 2.17 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

Data from ChEMBL 36 via Core Engine