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Compound Detail

CHEMBL4743243

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Cc1c([C@H](OC(C)(C)C)C(=O)O)c2n3cc(nc3c1CN(C)C)-c1cccc(c1)-c1cc(F)ccc1O[C@@H](C)CCCCOC1(C)CCN2CC1

Basic Information

ChEMBL ID CHEMBL4743243
Phase Preclinical
Structure Type MOL
InChI Key GJNGJGQODQELQP-HOYUZMNJSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

700.9
MW (Da)
8.44
ALogP
8
HBA
1
HBD
88.8
PSA (Ų)
0.22
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C41H53FN4O5
MW 700.90
Aromatic Rings 4
Heavy Atoms 51
NP-Likeness -0.45

Activity Summary

EC50 1 meas. best 8.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 8.36 8.36 4.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 4.4 nM 8.36 Allosteric inhibition of HIV-1 integrase assessed as antiviral activity against ... 32890685

Literature References

PubMed DOI Target Context # Activities
32890685 10.1016/j.bmcl.2020.127531 Unchecked 1
32890685 10.1016/j.bmcl.2020.127531 Nuclear receptor subfamily 1 group I member 2 1

Data from ChEMBL 36 via Core Engine