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Compound Detail

CHEMBL206509

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COC(=O)N[C@H](C(=O)NN(Cc1ccc(/C=C/c2ccccc2)cc1)C[C@@](O)(Cc1ccccc1)C(=O)N[C@H]1c2ccccc2C[C@H]1O)C(C)(C)C

Basic Information

ChEMBL ID CHEMBL206509
Phase Preclinical
Structure Type MOL
InChI Key MYCHAQXKDYLAGD-MDKKUHPCSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

704.9
MW (Da)
5.21
ALogP
7
HBA
5
HBD
140.2
PSA (Ų)
0.10
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C42H48N4O6
MW 704.87
Aromatic Rings 4
Heavy Atoms 52
NP-Likeness 0.07

Activity Summary

Ki 1 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
Ki 7.96 7.96 11.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Human immunodeficiency virus type 1 protease Ki = 11.0 nM 7.96 Inhibition of HIV1 protease 16509598

Literature References

PubMed DOI Target Context # Activities
16509598 10.1021/jm051239z Human immunodeficiency virus type 1 protease 1
16509598 10.1021/jm051239z MT4 1
16509598 10.1021/jm051239z Human immunodeficiency virus 1 1

Data from ChEMBL 36 via Core Engine