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Compound Detail

CHEMBL5641847

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Fc1ccccc1Cn1nc(-c2ccco2)cc1-c1ccccc1

Basic Information

ChEMBL ID CHEMBL5641847
Phase Preclinical
Structure Type MOL
InChI Key SGYHGRWAQXPRKW-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
4
Publications
0
Known Names

Molecular Properties

318.4
MW (Da)
5.00
ALogP
3
HBA
0
HBD
31.0
PSA (Ų)
0.53
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H15FN2O
MW 318.35
Aromatic Rings 4
Heavy Atoms 24
NP-Likeness -1.96

Activity Summary

IC50 1 meas. best 8.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neutrophil
CHEMBL5314326
IC50 8.04 8.04 9.1 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 961.67 ng.hr.mL-1 Mus musculus
CL 1.97 ml/min Mus musculus
T1/2 1.32 hr Mus musculus
Vz 225.0 ml Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neutrophil IC50 = 9.06 nM 8.04 Inhibition of fMLF/CB-induced human Neutrophil activation assessed as reduction ... 37918036

Literature References

PubMed DOI Target Context # Activities
37918036 10.1016/j.ejmech.2023.115874 Neutrophil 5
37918036 10.1016/j.ejmech.2023.115874 ADMET 4
37918036 10.1016/j.ejmech.2023.115874 3',5'-cyclic-AMP phosphodiesterase 4B 1
37918036 10.1016/j.ejmech.2023.115874 3',5'-cyclic-AMP phosphodiesterase 4D 1

Data from ChEMBL 36 via Core Engine