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Compound Detail

CHEMBL4780905

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Cn1c(C(=O)c2c[nH]c3c(F)cccc23)nc2ccc(F)cc21

Basic Information

ChEMBL ID CHEMBL4780905
Phase Preclinical
Structure Type MOL
InChI Key QLKHIHJMEWHCQU-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

311.3
MW (Da)
3.56
ALogP
3
HBA
1
HBD
50.7
PSA (Ų)
0.58
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 C17H11F2N3O
MW 311.29
Aromatic Rings 4
Heavy Atoms 23
NP-Likeness -1.27

Activity Summary

EC50 1 meas. best 9.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proprotein convertase subtilisin/kexin type 9
CHEMBL2929
EC50 9.82 9.82 0.1 1

Pharmacokinetic Data

Parameter Value Units Species
CL 41.7 mL.min-1.g-1 Mus musculus
CL 23.0 mL.min-1.g-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32823006 10.1016/j.ejmech.2020.112678 Proprotein convertase subtilisin/kexin type 9 3
32823006 10.1016/j.ejmech.2020.112678 ADMET 2
32823006 10.1016/j.ejmech.2020.112678 HepG2 1

Data from ChEMBL 36 via Core Engine