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Compound Detail

CHEMBL4551356

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O=C(O)c1[nH]c(-c2ccc(-c3nnn[nH]3)cc2C(F)(F)F)cc(=O)c1O

Basic Information

ChEMBL ID CHEMBL4551356
Phase Preclinical
Structure Type MOL
InChI Key CTOQHZRTEVUPLN-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

367.2
MW (Da)
1.64
ALogP
6
HBA
4
HBD
144.8
PSA (Ų)
0.55
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H8F3N5O4
MW 367.24
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -0.78

Activity Summary

IC50 2 meas. best 10.3
EC50 1 meas. best 4.94

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Polymerase acidic protein
CHEMBL1169598
IC50 10.3 8.815 0.1 2
Unchecked
CHEMBL612545
EC50 4.94 4.94 11500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31536340 10.1021/acs.jmedchem.9b00747 Polymerase acidic protein 3
31536340 10.1021/acs.jmedchem.9b00747 Unchecked 3
31536340 10.1021/acs.jmedchem.9b00747 Methionine aminopeptidase 2 1
31536340 10.1021/acs.jmedchem.9b00747 Arginase-1 1
31536340 10.1021/acs.jmedchem.9b00747 Carbonic anhydrase 2 1
31536340 10.1021/acs.jmedchem.9b00747 Macrophage metalloelastase 1
31536340 10.1021/acs.jmedchem.9b00747 MDCK 1
31536340 10.1021/acs.jmedchem.9b00747 NIH3T3 1

Data from ChEMBL 36 via Core Engine