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Compound Detail

CHEMBL431754

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CC(C)(C)NC(=O)[C@@H]1CC2CCCCC2CN1C[C@@H](O)[C@@H]1Cc2ccc(cc2)OCCOc2cc3ccccc3cc2C(=O)N[C@@H](CC(N)=O)C(=O)N1

Basic Information

ChEMBL ID CHEMBL431754
Phase Preclinical
Structure Type MOL
InChI Key BXXKSGNCOZTWCZ-BKGDRJHFSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

727.9
MW (Da)
3.47
ALogP
8
HBA
5
HBD
172.3
PSA (Ų)
0.26
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C41H53N5O7
MW 727.90
Aromatic Rings 3
Heavy Atoms 53
NP-Likeness 0.47

Activity Summary

EC50 1 meas. best 7.75
IC50 1 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
IC50 7.89 7.89 13.0 1
MT2
CHEMBL614184
EC50 7.75 7.75 18.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Human immunodeficiency virus type 1 protease IC50 = 13.0 nM 7.89 In vitro inhibition HIV-1 IIIB protease. -
MT2 EC50 = 18.0 nM 7.75 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