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Compound Detail

CHEMBL4741714

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C[C@@H]1C[C@H](N)C[C@H](c2ccccc2NC(=O)c2ccc(F)c(-c3c(F)cccc3F)n2)C1

Basic Information

ChEMBL ID CHEMBL4741714
Phase Preclinical
Structure Type MOL
InChI Key GAPPKQMJLOBLDJ-XHSDSOJGSA-N
1
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

439.5
MW (Da)
5.65
ALogP
3
HBA
2
HBD
68.0
PSA (Ų)
0.55
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24F3N3O
MW 439.48
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.62

Activity Summary

IC50 3 meas. best 10.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase pim-2
CHEMBL4523
IC50 10.74 10.74 0.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine/threonine-protein kinase pim-2 IC50 = 0.018 nM 10.74 Inhibition of PIM2 (unknown origin) 33128909

Literature References

PubMed DOI Target Context # Activities
33128909 10.1016/j.bmc.2020.115724 Serine/threonine-protein kinase pim-1 1
33128909 10.1016/j.bmc.2020.115724 Serine/threonine-protein kinase pim-2 1
33128909 10.1016/j.bmc.2020.115724 Serine/threonine-protein kinase pim-3 1

Data from ChEMBL 36 via Core Engine