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Compound Detail

CHEMBL4068343

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OC(Cn1cnnn1)(c1ccc(F)cc1F)C(F)(F)c1ccc(C#Cc2ccc(F)cc2)cn1

Basic Information

ChEMBL ID CHEMBL4068343
Phase Preclinical
Structure Type MOL
InChI Key BPGCIZWBROSBMV-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

471.4
MW (Da)
3.57
ALogP
6
HBA
1
HBD
76.7
PSA (Ų)
0.36
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H14F5N5O
MW 471.39
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.52

Activity Summary

IC50 2 meas. best 4.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 3A4
CHEMBL340
IC50 4.0 4.0 100000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cytochrome P450 3A4 IC50 = 100000.0 nM 4.0 Inhibition of CYP3A4 in human hepatocyte microsomes using testosterone substrate... 28651982

Literature References

PubMed DOI Target Context # Activities
28651982 10.1016/j.bmcl.2017.06.037 Lanosterol 14-alpha demethylase 6
28651982 10.1016/j.bmcl.2017.06.037 Cytochrome P450 3A4 2
37480712 10.1016/j.ejmech.2023.115658 Trichophyton rubrum 1

Data from ChEMBL 36 via Core Engine