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Compound Detail

CHEMBL3407856

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Cc1nc2ccc(-c3c(C)ccc(C(=O)c4c(-c5ccccc5)n(C)n(-c5ccccc5)c4=O)c3N)cc2s1

Basic Information

ChEMBL ID CHEMBL3407856
Phase Preclinical
Structure Type MOL
InChI Key CTFSTDZNMXJUAP-UHFFFAOYSA-N
2
Targets
6
Activities
2
Assay Types
4
PK Parameters
4
Publications
0
Known Names

Molecular Properties

530.6
MW (Da)
6.55
ALogP
7
HBA
1
HBD
82.9
PSA (Ų)
0.20
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H26N4O2S
MW 530.65
Aromatic Rings 6
Heavy Atoms 39
NP-Likeness -0.94

Activity Summary

IC50 5 meas. best 8.4
EC50 1 meas. best 6.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Eukaryotic translation initiation factor 2-alpha kinase 3
CHEMBL6030
IC50 8.4 7.22 4.0 4
Eukaryotic translation initiation factor 2-alpha kinase 3
CHEMBL6030
EC50 6.72 6.72 190.0 1
eIF-2-alpha kinase GCN2
CHEMBL5358
IC50 5.85 5.85 1400.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 53.06 ng.hr.mL-1 Rattus norvegicus
CL 23.33 mL.min-1.kg-1 Rattus norvegicus
F 3.0 % Rattus norvegicus
MRT 2.2 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