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Compound Detail

CHEMBL5091507

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C[C@@H]1Cc2nn3c(c2CN1C(=O)Nc1ccc(F)c(C(F)(F)F)c1)C(=O)N(C)O[C@@H](CO)C3

Basic Information

ChEMBL ID CHEMBL5091507
Phase Preclinical
Structure Type MOL
InChI Key ORJNUVVURQBJAG-ZYHUDNBSSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
3
Publications
0
Known Names

Molecular Properties

471.4
MW (Da)
2.40
ALogP
6
HBA
2
HBD
99.9
PSA (Ų)
0.66
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H21F4N5O4
MW 471.41
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.11

Activity Summary

EC50 1 meas. best 8.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Core antigen
CHEMBL1075091
EC50 8.57 8.57 2.7 1

Pharmacokinetic Data

Parameter Value Units Species
CL 7.2 mL.min-1.kg-1 Homo sapiens
CL 58.0 mL.min-1.kg-1 Mus musculus
CL 24.0 mL.min-1.kg-1 Rattus norvegicus
T1/2 1.6 hr Mus musculus
T1/2 1.4 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Core antigen EC50 = 2.7 nM 8.57 Modulation of capsid assembly in HBV infected in human HepG2.2.15 cells assessed... 34492302

Literature References

PubMed DOI Target Context # Activities
34492302 10.1016/j.bmcl.2021.128353 ADMET 7
34492302 10.1016/j.bmcl.2021.128353 Core antigen 1
34492302 10.1016/j.bmcl.2021.128353 No relevant target 1

Data from ChEMBL 36 via Core Engine