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Compound Detail

CHEMBL383077

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Cc1cc2c(F)c(Oc3ncnn4cc(OCCCS(C)(=O)=O)c(C)c34)ccc2[nH]1

Basic Information

ChEMBL ID CHEMBL383077
Phase Preclinical
Structure Type MOL
InChI Key DZEADOQXGYJGID-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

432.5
MW (Da)
3.57
ALogP
7
HBA
1
HBD
98.6
PSA (Ų)
0.45
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H21FN4O4S
MW 432.48
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.15

Activity Summary

IC50 3 meas. best 7.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.16 7.16 70.0 1
Cytochrome P450 3A4
CHEMBL340
IC50 4.77 4.77 17000.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 4.7 4.7 20000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 80008.8 ng.hr.mL-1 Mus musculus
Cmax 57000.0 nM Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16570908 10.1021/jm051106d Mus musculus 2
16570908 10.1021/jm051106d Vascular endothelial growth factor receptor 2 1
16570908 10.1021/jm051106d Cytochrome P450 3A4 1
16570908 10.1021/jm051106d Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine