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Compound Detail

CHEMBL5187784

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COc1cccc2[nH]c(C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C[C@@H]3CCCNC3=O)C(=O)COC(=O)c3ccccn3)cc12

Basic Information

ChEMBL ID CHEMBL5187784
Phase Preclinical
Structure Type MOL
InChI Key PFYSTXWNQVFKTC-IGKWTDBASA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

591.7
MW (Da)
2.54
ALogP
8
HBA
4
HBD
168.6
PSA (Ų)
0.22
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H37N5O7
MW 591.67
Aromatic Rings 3
Heavy Atoms 43
NP-Likeness -0.32

Activity Summary

IC50 1 meas. best 6.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Replicase polyprotein 1ab
CHEMBL4523582
IC50 6.9 6.9 125.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Replicase polyprotein 1ab IC50 = 125.5 nM 6.9 Inhibition of SARS-CoV-2 3CL protease incubated for 30 mins by FRET assay 34242027

Literature References

PubMed DOI Target Context # Activities
34242027 10.1021/acs.jmedchem.1c00616 Replicase polyprotein 1ab 1
34242027 10.1021/acs.jmedchem.1c00616 SARS-CoV-2 1
34242027 10.1021/acs.jmedchem.1c00616 No relevant target 1

Data from ChEMBL 36 via Core Engine