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Compound Detail

CHEMBL4874709

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NCc1ccc2c(c1)nc(CN1C(=O)C3(CC3)c3ccc(F)cc31)n2C1CCOCC1

Basic Information

ChEMBL ID CHEMBL4874709
Phase Preclinical
Structure Type MOL
InChI Key UGTWLLBIEDUTMG-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
21
PK Parameters
5
Publications
0
Known Names

Molecular Properties

420.5
MW (Da)
3.56
ALogP
5
HBA
1
HBD
73.4
PSA (Ų)
0.70
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H25FN4O2
MW 420.49
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.01

Activity Summary

EC50 1 meas. best 8.62
IC50 1 meas. best 8.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fusion glycoprotein F0
CHEMBL3856166
IC50 8.92 8.92 1.2 1
Human orthopneumovirus
CHEMBL613127
EC50 8.62 8.62 2.4 1

Pharmacokinetic Data

Parameter Value Units Species
CL 58.0 mL.min-1.kg-1 Mus musculus
CL 19.2 mL.min-1.kg-1 Canis lupus familiaris
Cmax 1070.18 nM Mus musculus
Cmax 1200.98 nM Canis lupus familiaris
F 39.4 % Mus musculus
F 163.0 % Canis lupus familiaris
Fu 0.399 - Rattus norvegicus
Fu 0.497 - Canis lupus familiaris
Fu 0.548 - Homo sapiens
T1/2 4.1 hr Rattus norvegicus
T1/2 4.1 hr Canis lupus familiaris
T1/2 0.3483 hr Homo sapiens
T1/2 1.023 hr Rattus norvegicus
T1/2 16.67 hr Canis lupus familiaris
T1/2 3.283 hr Homo sapiens
T1/2 1.7 hr Mus musculus
T1/2 5.2 hr Canis lupus familiaris
T1/2 1.4 hr Mus musculus
T1/2 3.1 hr Canis lupus familiaris
Tmax 1.7 hr Mus musculus
Tmax 0.5 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33729773 10.1021/acs.jmedchem.0c01882 ADMET 31
33729773 10.1021/acs.jmedchem.0c01882 Fusion glycoprotein F0 1
33729773 10.1021/acs.jmedchem.0c01882 No relevant target 1
33729773 10.1021/acs.jmedchem.0c01882 HepG2 1
33729773 10.1021/acs.jmedchem.0c01882 Human orthopneumovirus 1

Data from ChEMBL 36 via Core Engine