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Compound Detail

CHEMBL4093499

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O=C(NCc1ccc(C(F)(F)F)cc1)c1cccc(CN2CCCCC2)c1

Basic Information

ChEMBL ID CHEMBL4093499
Phase Preclinical
Structure Type MOL
InChI Key DZKGORBEITZGMV-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

376.4
MW (Da)
4.62
ALogP
2
HBA
1
HBD
32.3
PSA (Ų)
0.83
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23F3N2O
MW 376.42
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -1.68

Activity Summary

EC50 1 meas. best 7.52
IC50 1 meas. best 7.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
INS1
CHEMBL613545
EC50 7.52 7.52 30.0 1
Eukaryotic translation initiation factor 2-alpha kinase 3
CHEMBL4105946
IC50 7.43 7.43 37.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28696115 10.1021/acs.jmedchem.7b00435 INS1 16
28696115 10.1021/acs.jmedchem.7b00435 Mus musculus 6
28696115 10.1021/acs.jmedchem.7b00435 Eukaryotic translation initiation factor 2-alpha kinase 3 4
28696115 10.1021/acs.jmedchem.7b00435 Beta-TC6 2
28696115 10.1021/acs.jmedchem.7b00435 Unchecked 2
28696115 10.1021/acs.jmedchem.7b00435 Cyclic AMP-dependent transcription factor ATF-6 alpha 2

Data from ChEMBL 36 via Core Engine