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Compound Detail

CHEMBL3623135

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Nc1ncc(C(=O)NC2CC2)c2ccc(-c3cccc(F)c3)nc12

Basic Information

ChEMBL ID CHEMBL3623135
Phase Preclinical
Structure Type MOL
InChI Key XWLOYAAKIFUZDU-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

322.3
MW (Da)
2.91
ALogP
4
HBA
2
HBD
80.9
PSA (Ų)
0.78
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H15FN4O
MW 322.34
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.48

Activity Summary

IC50 2 meas. best 10.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HUVEC
CHEMBL613979
IC50 10.0 10.0 0.1 1
Mitogen-activated protein kinase kinase kinase kinase 4
CHEMBL6166
IC50 8.85 8.85 1.4 1

Pharmacokinetic Data

Parameter Value Units Species
CL 16.0 mL.min-1.kg-1 Homo sapiens
CL 78.0 mL.min-1.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26288693 10.1021/acsmedchemlett.5b00174 MDCK 2
26288693 10.1021/acsmedchemlett.5b00174 Mitogen-activated protein kinase kinase kinase kinase 4 1
26288693 10.1021/acsmedchemlett.5b00174 HUVEC 1
26288693 10.1021/acsmedchemlett.5b00174 Liver microsome 1
26288693 10.1021/acsmedchemlett.5b00174 Liver 1

Data from ChEMBL 36 via Core Engine