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Compound Detail

CHEMBL4848804

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COc1ncc(-c2cnc3[nH]cc(C(=O)c4cccc(NS(=O)(=O)Cc5ccccc5)c4F)c3c2)cn1

Basic Information

ChEMBL ID CHEMBL4848804
Phase Preclinical
Structure Type MOL
InChI Key VNUCFYAGMGVERJ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

517.5
MW (Da)
4.34
ALogP
7
HBA
2
HBD
126.9
PSA (Ų)
0.29
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H20FN5O4S
MW 517.54
Aromatic Rings 5
Heavy Atoms 37
NP-Likeness -1.16

Activity Summary

Kd 1 meas. best 9.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dual specificity mitogen-activated protein kinase kinase 4
CHEMBL2201
Kd 9.07 9.07 0.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33199152 10.1016/j.ejmech.2020.112963 Dual specificity mitogen-activated protein kinase kinase 4 2
33199152 10.1016/j.ejmech.2020.112963 Serine/threonine-protein kinase B-raf 1
33199152 10.1016/j.ejmech.2020.112963 Mitogen-activated protein kinase kinase kinase kinase 5 1
33199152 10.1016/j.ejmech.2020.112963 Dual specificity mitogen-activated protein kinase kinase 7 1
33199152 10.1016/j.ejmech.2020.112963 Mitogen-activated protein kinase 8 1
33199152 10.1016/j.ejmech.2020.112963 Mitogen-activated protein kinase kinase kinase 20 1

Data from ChEMBL 36 via Core Engine