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Compound Detail

CHEMBL3337533

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O=C(N[C@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccncc1)c1ccc(-c2ccc(OCc3ccc(F)cc3)c(F)c2)cc1F

Basic Information

ChEMBL ID CHEMBL3337533
Phase Preclinical
Structure Type MOL
InChI Key POKFDWANZDIRIE-MGBGTMOVSA-N
2
Targets
2
Activities
2
Assay Types
3
PK Parameters
14
Publications
0
Known Names

Molecular Properties

620.6
MW (Da)
7.21
ALogP
4
HBA
3
HBD
96.1
PSA (Ų)
0.15
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H27F3N4O3
MW 620.63
Aromatic Rings 6
Heavy Atoms 46
NP-Likeness -1.11

Activity Summary

EC50 1 meas. best 6.55
Kd 1 meas. best 5.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma cruzi
CHEMBL368
EC50 6.55 6.55 280.0 1
Sterol 14-alpha demethylase
CHEMBL1075110
Kd 5.89 5.89 1300.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.25 hr Homo sapiens
T1/2 0.65 hr Rattus norvegicus
T1/2 1.117 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25101801 10.1021/jm500448u Trypanosoma cruzi 4
25101801 10.1021/jm500448u ADMET 4
25101801 10.1021/jm500448u Liver 3
25101801 10.1021/jm500448u Liver microsome 2
25101801 10.1021/jm500448u Intestine 2
25101801 10.1021/jm500448u Lung 2
25101801 10.1021/jm500448u Heart 2
25101801 10.1021/jm500448u Cytochrome P450 1A2 1
25101801 10.1021/jm500448u Cytochrome P450 2C9 1
25101801 10.1021/jm500448u Cytochrome P450 2D6 1
25101801 10.1021/jm500448u Cytochrome P450 3A4 1
25101801 10.1021/jm500448u C2C12 1
25101801 10.1021/jm500448u Sterol 14-alpha demethylase 1
25101801 10.1021/jm500448u Unchecked 1

Data from ChEMBL 36 via Core Engine