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Compound Detail

CHEMBL242137

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CN1C[C@H](O)C[C@H]1c1nc(C(=O)NCc2ccc(F)cc2)c(O)c(=O)n1C

Basic Information

ChEMBL ID CHEMBL242137
Phase Preclinical
Structure Type MOL
InChI Key OAMCENINXMAPLY-OLZOCXBDSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
4
Publications
0
Known Names

Molecular Properties

376.4
MW (Da)
0.29
ALogP
7
HBA
3
HBD
107.7
PSA (Ų)
0.71
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H21FN4O4
MW 376.39
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.66

Activity Summary

IC50 1 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 integrase
CHEMBL3471
IC50 7.0 7.0 100.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 37.64 ng.hr.mL-1 Rattus norvegicus
CL 21.0 mL.min-1.kg-1 Rattus norvegicus
F 2.0 % Rattus norvegicus
T1/2 1.8 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17824681 10.1021/jm0704705 Rattus norvegicus 4
17824681 10.1021/jm0704705 Human immunodeficiency virus 1 2
17824681 10.1021/jm0704705 Plasma 2
17824681 10.1021/jm0704705 Human immunodeficiency virus type 1 integrase 1

Data from ChEMBL 36 via Core Engine