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Compound Detail

CHEMBL5558861

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C=CC(=O)Nc1cc(Cn2nnc3c(C(=O)NCC4CC(F)(F)C4)cccc32)ccc1F

Basic Information

ChEMBL ID CHEMBL5558861
Phase Preclinical
Structure Type MOL
InChI Key LJQGHKNSFBSZFJ-UHFFFAOYSA-N
7
Targets
7
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

443.4
MW (Da)
3.52
ALogP
5
HBA
2
HBD
88.9
PSA (Ų)
0.55
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H20F3N5O2
MW 443.43
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.52

Activity Summary

IC50 7 meas. best 8.88

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 8.88 8.88 1.3 1
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 8.54 8.54 2.9 1
KYSE-150 cell line
CHEMBL613998
IC50 5.16 5.16 6860.0 1
MDA-MB-231
CHEMBL400
IC50 5.0 5.0 10030.0 1
MDA-MB-435
CHEMBL614697
IC50 4.57 4.57 26960.0 1
HepG2
CHEMBL395
IC50 4.53 4.53 29580.0 1
HUVEC
CHEMBL613979
IC50 4.34 4.34 46180.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38643670 10.1016/j.ejmech.2024.116415 Fibroblast growth factor receptor 1 1
38643670 10.1016/j.ejmech.2024.116415 Fibroblast growth factor receptor 4 1
38643670 10.1016/j.ejmech.2024.116415 Unchecked 1
38643670 10.1016/j.ejmech.2024.116415 MDA-MB-435 1
38643670 10.1016/j.ejmech.2024.116415 MDA-MB-231 1
38643670 10.1016/j.ejmech.2024.116415 KYSE-150 cell line 1
38643670 10.1016/j.ejmech.2024.116415 HepG2 1
38643670 10.1016/j.ejmech.2024.116415 HUVEC 1

Data from ChEMBL 36 via Core Engine