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Compound Detail

CHEMBL244764

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CC(=O)c1cccc(N2C[C@@H](C(=O)N[C@@H](Cc3ccccc3)[C@@H](O)CN(Cc3ccc(-c4ccccn4)cc3)NC(=O)[C@@H]3CN(c4cccc(C(C)=O)c4)C(=O)O3)OC2=O)c1

Basic Information

ChEMBL ID CHEMBL244764
Phase Preclinical
Structure Type MOL
InChI Key BEQKYIIVCGSEAQ-IWWWZYECSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

824.9
MW (Da)
5.13
ALogP
11
HBA
3
HBD
187.8
PSA (Ų)
0.09
QED
3
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C46H44N6O9
MW 824.89
Aromatic Rings 5
Heavy Atoms 61
NP-Likeness -0.52

Activity Summary

Ki 1 meas. best 5.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protease
CHEMBL2366517
Ki 5.96 5.96 1090.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protease Ki = 1090.0 nM 5.96 Inhibition of Wild type HIV1 Protease by FRET based assay 17696512

Literature References

PubMed DOI Target Context # Activities
17696512 10.1021/jm070284z Protease 1

Data from ChEMBL 36 via Core Engine