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Compound Detail

CHEMBL2171126

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Cn1cc(-c2ccc3c(c2)CCN3C(=O)Cc2cc(F)cc(F)c2F)c2c(N)ncnc21

Basic Information

ChEMBL ID CHEMBL2171126
Phase Preclinical
Structure Type MOL
InChI Key JCUSVFKWUQBVHH-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

437.4
MW (Da)
3.77
ALogP
5
HBA
1
HBD
77.0
PSA (Ų)
0.50
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H18F3N5O
MW 437.43
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.25

Activity Summary

IC50 2 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Eukaryotic translation initiation factor 2-alpha kinase 3
CHEMBL6030
IC50 9.7 8.61 0.2 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22827572 10.1021/jm300713s Eukaryotic translation initiation factor 2-alpha kinase 3 2
- 10.6019/CHEMBL3988181 Unchecked 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek1 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek2 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek3 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek4 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek5 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek6 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek7 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek9 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek10 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek11 1

Data from ChEMBL 36 via Core Engine