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Compound Detail

CHEMBL3407846

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Cn1cc(-c2ccc3c(c2)CCN3CC(=O)c2cc(F)cc(C(F)(F)F)c2)c2c(N)ncnc21

Basic Information

ChEMBL ID CHEMBL3407846
Phase Preclinical
Structure Type MOL
InChI Key ZWDWGLVLLJCBMR-UHFFFAOYSA-N
2
Targets
5
Activities
2
Assay Types
4
PK Parameters
4
Publications
0
Known Names

Molecular Properties

469.4
MW (Da)
4.62
ALogP
6
HBA
1
HBD
77.0
PSA (Ų)
0.35
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 C24H19F4N5O
MW 469.44
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.14

Activity Summary

IC50 4 meas. best 9.0
EC50 1 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Eukaryotic translation initiation factor 2-alpha kinase 3
CHEMBL6030
IC50 9.0 8.3067 1.0 3
Eukaryotic translation initiation factor 2-alpha kinase 3
CHEMBL6030
EC50 7.89 7.89 13.0 1
eIF-2-alpha kinase GCN2
CHEMBL5358
IC50 5.41 5.41 3900.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 3849.41 ng.hr.mL-1 Rattus norvegicus
CL 4.833 mL.min-1.kg-1 Rattus norvegicus
F 44.0 % Rattus norvegicus
MRT 3.7 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25587754 10.1021/jm5017494 Eukaryotic translation initiation factor 2-alpha kinase 3 6
25587754 10.1021/jm5017494 Rattus norvegicus 5
25587754 10.1021/jm5017494 eIF-2-alpha kinase GCN2 1
25587754 10.1021/jm5017494 Serine/threonine-protein kinase B-raf 1

Data from ChEMBL 36 via Core Engine