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Compound Detail

CHEMBL4640881

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CN1CCN(c2cc(-c3ccncc3)c(-c3ccc4ccc(F)cc4c3)nn2)CC1

Basic Information

ChEMBL ID CHEMBL4640881
Phase Preclinical
Structure Type MOL
InChI Key JFIFTUZQRREXAJ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

399.5
MW (Da)
4.25
ALogP
5
HBA
0
HBD
45.1
PSA (Ų)
0.52
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H22FN5
MW 399.47
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.35

Activity Summary

IC50 2 meas. best 6.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 14
CHEMBL260
IC50 6.15 6.15 710.0 1
Mitogen-activated protein kinase 11
CHEMBL3961
IC50 5.58 5.58 2600.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.8667 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase 14 IC50 = 710.0 nM 6.15 Inhibition of human p38alpha 30978288
Mitogen-activated protein kinase 11 IC50 = 2600.0 nM 5.58 Inhibition of human p38beta 30978288

Literature References

PubMed DOI Target Context # Activities
30978288 10.1021/acs.jmedchem.9b00058 Mitogen-activated protein kinase 14 1
30978288 10.1021/acs.jmedchem.9b00058 Mitogen-activated protein kinase 11 1
30978288 10.1021/acs.jmedchem.9b00058 Casein kinase I isoform delta 1
30978288 10.1021/acs.jmedchem.9b00058 ADMET 1

Data from ChEMBL 36 via Core Engine