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Compound Detail

CHEMBL72474

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CC(=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 CHEMBL72474
Phase Preclinical
Structure Type MOL
InChI Key YDVBUHNKHQLBCZ-PWYSEMTOSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

542.8
MW (Da)
3.03
ALogP
5
HBA
4
HBD
110.8
PSA (Ų)
0.36
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H50N4O4
MW 542.77
Aromatic Rings 1
Heavy Atoms 39
NP-Likeness 0.16

Activity Summary

EC50 1 meas. best 7.54
IC50 1 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
IC50 8.52 8.52 3.0 1
MT2
CHEMBL614184
EC50 7.54 7.54 29.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Human immunodeficiency virus type 1 protease IC50 = 3.0 nM 8.52 In vitro inhibition HIV-1 IIIB protease. -
MT2 EC50 = 29.0 nM 7.54 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