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Compound Detail

CHEMBL4096118

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

Basic Information

ChEMBL ID CHEMBL4096118
Phase Preclinical
Structure Type MOL
InChI Key VDNSLSLDVQPTPX-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

550.4
MW (Da)
4.40
ALogP
7
HBA
2
HBD
88.8
PSA (Ų)
0.26
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H17F7N6O
MW 550.44
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.62

Activity Summary

IC50 1 meas. best 5.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 3A4
CHEMBL340
IC50 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cytochrome P450 3A4 IC50 = 10000.0 nM 5.0 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 2
28651982 10.1016/j.bmcl.2017.06.037 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine