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Compound Detail

CHEMBL431387

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CC(C)[C@@H]1NC(=O)CCCCCCCOc2ccc(cc2)C[C@@H]([C@H](O)CN2CC3CCCCC3C[C@H]2C(=O)NC(C)(C)C)NC1=O

Basic Information

ChEMBL ID CHEMBL431387
Phase Preclinical
Structure Type MOL
InChI Key WEDYIPBWZKOBFA-ZUCIFVEUSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

640.9
MW (Da)
4.74
ALogP
6
HBA
4
HBD
120.0
PSA (Ų)
0.37
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C37H60N4O5
MW 640.91
Aromatic Rings 1
Heavy Atoms 46
NP-Likeness 0.76

Activity Summary

EC50 1 meas. best 7.58
IC50 1 meas. best 8.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
IC50 8.47 8.47 3.4 1
MT2
CHEMBL614184
EC50 7.58 7.58 26.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Human immunodeficiency virus type 1 protease IC50 = 3.4 nM 8.47 In vitro inhibition HIV-1 IIIB protease. -
MT2 EC50 = 26.0 nM 7.58 Effective concentration against HIV infected MT-2 cell line -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(00)80074-8 Human immunodeficiency virus type 1 protease 1
- 10.1016/S0960-894X(00)80074-8 MT2 1

Data from ChEMBL 36 via Core Engine