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Compound Detail

CHEMBL5189372

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CNC(=O)[C@]1(C)CC[C@@H](Nc2ncc3c(Br)nn(-c4ccc(-c5nnc(C)s5)c(CC#N)c4)c3n2)C1

Basic Information

ChEMBL ID CHEMBL5189372
Phase Preclinical
Structure Type MOL
InChI Key KFAZKKZRIOFNKG-OYLFLEFRSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

566.5
MW (Da)
4.19
ALogP
10
HBA
2
HBD
134.3
PSA (Ų)
0.36
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H24BrN9OS
MW 566.49
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.11

Activity Summary

IC50 1 meas. best 7.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
eIF-2-alpha kinase GCN2
CHEMBL5358
IC50 7.11 7.11 78.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
eIF-2-alpha kinase GCN2 IC50 = 78.0 nM 7.11 Inhibition of GCN2 (unknown origin) 36127295

Literature References

PubMed DOI Target Context # Activities
36127295 10.1021/acs.jmedchem.2c00736 eIF-2-alpha kinase GCN2 2

Data from ChEMBL 36 via Core Engine