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Compound Detail

CHEMBL5194822

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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)C(C)(C)C#N)cc12

Basic Information

ChEMBL ID CHEMBL5194822
Phase Preclinical
Structure Type MOL
InChI Key XQNMIBIMRDZGLC-NYVOZVTQSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

581.7
MW (Da)
2.38
ALogP
8
HBA
4
HBD
179.5
PSA (Ų)
0.26
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H39N5O7
MW 581.67
Aromatic Rings 2
Heavy Atoms 42
NP-Likeness -0.07

Activity Summary

IC50 1 meas. best 7.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Replicase polyprotein 1ab
CHEMBL4523582
IC50 7.66 7.66 21.9 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.25 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Replicase polyprotein 1ab IC50 = 21.9 nM 7.66 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 ADMET 2
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