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Compound Detail

CHEMBL5220178

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COc1cc(C#N)c(Oc2ccccc2C)cc1-n1c(=O)cc(C(F)(F)F)[nH]c1=O

Basic Information

ChEMBL ID CHEMBL5220178
Phase Preclinical
Structure Type MOL
InChI Key GSEHYSQYWAECFH-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

417.3
MW (Da)
3.53
ALogP
6
HBA
1
HBD
97.1
PSA (Ų)
0.70
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H14F3N3O4
MW 417.34
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.07

Activity Summary

IC50 2 meas. best 6.79

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Branched-chain-amino-acid aminotransferase, mitochondrial
CHEMBL3616354
IC50 6.79 6.79 162.0 1
Branched-chain-amino-acid aminotransferase, cytosolic
CHEMBL4679
IC50 6.79 6.79 162.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
36261130 10.1021/acs.jmedchem.2c00441 ADMET 2
36261130 10.1021/acs.jmedchem.2c00441 Branched-chain-amino-acid aminotransferase, cytosolic 1
36261130 10.1021/acs.jmedchem.2c00441 Branched-chain-amino-acid aminotransferase, mitochondrial 1
36261130 10.1021/acs.jmedchem.2c00441 No relevant target 1

Data from ChEMBL 36 via Core Engine