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Compound Detail

CHEMBL3407849

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CNc1ncc2ccc(Oc3cc(C(=O)c4c(-c5ccccc5)n(C)n(-c5ccccc5)c4=O)ccc3C)cc2n1

Basic Information

ChEMBL ID CHEMBL3407849
Phase Preclinical
Structure Type MOL
InChI Key QLCVZRYQHBSADC-UHFFFAOYSA-N
3
Targets
7
Activities
2
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

541.6
MW (Da)
6.16
ALogP
8
HBA
1
HBD
91.0
PSA (Ų)
0.24
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H27N5O3
MW 541.61
Aromatic Rings 6
Heavy Atoms 41
NP-Likeness -0.84

Activity Summary

IC50 6 meas. best 9.0
EC50 1 meas. best 6.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Eukaryotic translation initiation factor 2-alpha kinase 3
CHEMBL6030
IC50 9.0 7.2825 1.0 4
eIF-2-alpha kinase GCN2
CHEMBL5358
IC50 8.3 8.3 5.0 1
Serine/threonine-protein kinase B-raf
CHEMBL5145
IC50 8.1 8.1 8.0 1
Eukaryotic translation initiation factor 2-alpha kinase 3
CHEMBL6030
EC50 6.51 6.51 310.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 497.0 mL.min-1.g-1 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 eIF-2-alpha kinase GCN2 1
25587754 10.1021/jm5017494 Serine/threonine-protein kinase B-raf 1
25587754 10.1021/jm5017494 ADMET 1

Data from ChEMBL 36 via Core Engine