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Compound Detail

CHEMBL7447

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C=C(C)[C@@H]1CC[C@]2(C(=O)NCCCCCCCC(=O)N[C@@H](CC(C)C)[C@@H](O)CC(=O)O)CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@H](O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12

Basic Information

ChEMBL ID CHEMBL7447
Phase Preclinical
Structure Type MOL
InChI Key SPZFCKVVHXRLAI-XOCWCZJOSA-N
2
Targets
7
Activities
2
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

755.1
MW (Da)
8.83
ALogP
5
HBA
5
HBD
136.0
PSA (Ų)
0.08
QED
2
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C46H78N2O6
MW 755.14
Aromatic Rings 0
Heavy Atoms 54
NP-Likeness 1.96

Activity Summary

IC50 5 meas. best 7.52
EC50 2 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus 1
CHEMBL378
IC50 7.52 6.24 30.0 4
H9
CHEMBL614806
EC50 7.52 7.52 30.0 1
Human immunodeficiency virus 1
CHEMBL378
EC50 6.48 6.48 329.6 1
H9
CHEMBL614806
IC50 5.57 5.57 2700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35513221 10.1016/j.bmcl.2022.128768 Human immunodeficiency virus 1 3
8676334 10.1021/jm950922q H9 2
8676334 10.1021/jm950922q Human immunodeficiency virus type 1 protease 1
8676334 10.1021/jm950922q Human immunodeficiency virus 1 1
- 10.1007/s00044-010-9467-2 ADMET 1
- 10.1007/s00044-010-9467-2 Human immunodeficiency virus 1 1
33201699 10.1021/acs.jmedchem.0c01348 Human immunodeficiency virus 1 1
35513221 10.1016/j.bmcl.2022.128768 TZM 1
35513221 10.1016/j.bmcl.2022.128768 ADMET 1

Data from ChEMBL 36 via Core Engine