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Compound Detail

CHEMBL1952125

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FC(F)(F)Oc1cccc(-n2nnc3ccc(NC4CC5(CCNCC5)C4)nc32)c1

Basic Information

ChEMBL ID CHEMBL1952125
Phase Preclinical
Structure Type MOL
InChI Key NRHBVVQSMCFGOS-UHFFFAOYSA-N
4
Targets
5
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

418.4
MW (Da)
3.66
ALogP
7
HBA
2
HBD
76.9
PSA (Ų)
0.67
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 C20H21F3N6O
MW 418.42
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.26

Activity Summary

IC50 4 meas. best 7.96
EC50 1 meas. best 6.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase pim-1
CHEMBL2147
IC50 7.96 7.96 11.0 1
Serine/threonine-protein kinase pim-3
CHEMBL5407
IC50 7.64 7.64 23.0 1
Serine/threonine-protein kinase pim-2
CHEMBL4523
IC50 6.66 6.66 218.0 1
Serine/threonine-protein kinase pim-1
CHEMBL2147
EC50 6.23 6.23 590.0 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 6.11 6.11 778.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22266039 10.1016/j.bmcl.2011.12.130 Serine/threonine-protein kinase pim-1 2
22266039 10.1016/j.bmcl.2011.12.130 Serine/threonine-protein kinase pim-2 1
22266039 10.1016/j.bmcl.2011.12.130 Serine/threonine-protein kinase pim-3 1
22266039 10.1016/j.bmcl.2011.12.130 Receptor-type tyrosine-protein kinase FLT3 1

Data from ChEMBL 36 via Core Engine