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Compound Detail

CHEMBL4638092

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Cc1cn(-c2cc(NC(=O)c3ccc(C)c(Oc4ccccc4)c3)cc(C(F)(F)F)c2)cn1

Basic Information

ChEMBL ID CHEMBL4638092
Phase Preclinical
Structure Type MOL
InChI Key ZPPJQUHJUSSFKP-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
5
PK Parameters
6
Publications
0
Known Names

Molecular Properties

451.4
MW (Da)
6.55
ALogP
4
HBA
1
HBD
56.1
PSA (Ų)
0.37
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H20F3N3O2
MW 451.45
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.59

Activity Summary

IC50 2 meas. best 6.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mast/stem cell growth factor receptor Kit
CHEMBL1936
IC50 6.21 6.21 618.0 1
PCSK9/LDLR
CHEMBL4523996
IC50 4.87 4.87 13400.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 508.0 ng.hr.mL-1 Mus musculus
AUC 541.0 ng.hr.mL-1 Mus musculus
CL 12.47 mL.min-1.kg-1 Mus musculus
MRT 2.27 hr Mus musculus
T1/2 2.15 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32051094 10.1016/j.bmc.2020.115344 ADMET 6
32051094 10.1016/j.bmc.2020.115344 PCSK9/LDLR 1
32051094 10.1016/j.bmc.2020.115344 Mast/stem cell growth factor receptor Kit 1
32051094 10.1016/j.bmc.2020.115344 Tyrosine-protein kinase ABL1 1
32051094 10.1016/j.bmc.2020.115344 Platelet-derived growth factor receptor beta 1
32051094 10.1016/j.bmc.2020.115344 Proto-oncogene tyrosine-protein kinase Src 1

Data from ChEMBL 36 via Core Engine