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Compound Detail

CHEMBL3414914

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COc1cnc2ccc(C(F)(F)c3nnc4c(F)cc(-c5cscn5)cn34)cc2c1

Basic Information

ChEMBL ID CHEMBL3414914
Phase Preclinical
Structure Type MOL
InChI Key PKBNSFDYLATYAR-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
4
PK Parameters
5
Publications
0
Known Names

Molecular Properties

427.4
MW (Da)
4.69
ALogP
7
HBA
0
HBD
65.2
PSA (Ų)
0.42
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H12F3N5OS
MW 427.41
Aromatic Rings 5
Heavy Atoms 30
NP-Likeness -1.61

Activity Summary

IC50 2 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hepatocyte growth factor receptor
CHEMBL3717
IC50 8.7 8.425 2.0 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 2778.16 ng.hr.mL-1 Rattus norvegicus
CL 1.5 mL.min-1.kg-1 Rattus norvegicus
F 9.0 % Rattus norvegicus
T1/2 1.5 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25699405 10.1021/jm501913a Rattus norvegicus 5
25699405 10.1021/jm501913a Liver microsome 2
25699405 10.1021/jm501913a Hepatocyte growth factor receptor 2
25699405 10.1021/jm501913a Cytochrome P450 2D6 1
25699405 10.1021/jm501913a Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine