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Compound Detail

CHEMBL101560

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O=C(N[C@@H](Cc1ccccc1)[C@@H](O)C[C@@H](Cc1ccccc1)C(=O)N[C@H]1c2ccccc2C[C@H]1O)OC1CCCC1

Basic Information

ChEMBL ID CHEMBL101560
Phase Preclinical
Structure Type MOL
InChI Key UMNROTOYYWSPDV-KHQGQIEXSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

556.7
MW (Da)
4.65
ALogP
5
HBA
4
HBD
107.9
PSA (Ų)
0.28
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H40N2O5
MW 556.70
Aromatic Rings 3
Heavy Atoms 41
NP-Likeness 0.44

Activity Summary

IC50 2 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protease
CHEMBL2366517
IC50 9.52 9.52 0.3 1
Human immunodeficiency virus type 1 protease
CHEMBL243
IC50 9.48 9.48 0.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protease IC50 = 0.3 nM 9.52 Inhibition of HIV1 protease 19323561
Human immunodeficiency virus type 1 protease IC50 = 0.33 nM 9.48 Inhibition of HIV-1 protease 8423600

Literature References

PubMed DOI Target Context # Activities
8423600 10.1021/jm00054a015 Human immunodeficiency virus type 1 protease 2
19323561 10.1021/jm900064c Protease 1
19323561 10.1021/jm900064c Human immunodeficiency virus 1 1

Data from ChEMBL 36 via Core Engine