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Compound Detail

CHEMBL4553669

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O=C(CF)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1cnnc2ccccc12

Basic Information

ChEMBL ID CHEMBL4553669
Phase Preclinical
Structure Type MOL
InChI Key JTZHZTGBVTUESQ-IBGZPJMESA-N
1
Targets
2
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

394.4
MW (Da)
1.63
ALogP
5
HBA
2
HBD
101.0
PSA (Ų)
0.60
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H19FN4O3
MW 394.41
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.79

Activity Summary

IC50 2 meas. best 6.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cysteine protease ATG4B
CHEMBL1741221
IC50 6.72 6.68 190.0 2

Pharmacokinetic Data

Parameter Value Units Species
CL 9.9 mL.min-1.kg-1 Homo sapiens
CL 39.0 mL.min-1.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27563406 10.1021/acsmedchemlett.6b00208 Cysteine protease ATG4B 2
27563406 10.1021/acsmedchemlett.6b00208 ADMET 2
27563406 10.1021/acsmedchemlett.6b00208 HEK-293T 1
27563406 10.1021/acsmedchemlett.6b00208 No relevant target 1

Data from ChEMBL 36 via Core Engine