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Compound Detail

CHEMBL305463

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CCCCCCC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)[C@H](O)CN1CC2CCCCC2C[C@H]1C(=O)NC(C)(C)C)C(C)C

Basic Information

ChEMBL ID CHEMBL305463
Phase Preclinical
Structure Type MOL
InChI Key DUTCXSHILPDZPT-XQEBEITKSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

612.9
MW (Da)
4.98
ALogP
5
HBA
4
HBD
110.8
PSA (Ų)
0.21
QED
1
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H60N4O4
MW 612.90
Aromatic Rings 1
Heavy Atoms 44
NP-Likeness 0.17

Activity Summary

EC50 1 meas. best 6.42
IC50 1 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
IC50 8.22 8.22 6.0 1
MT2
CHEMBL614184
EC50 6.42 6.42 378.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Human immunodeficiency virus type 1 protease IC50 = 6.0 nM 8.22 In vitro inhibition HIV-1 IIIB protease. -
MT2 EC50 = 378.0 nM 6.42 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