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Compound Detail

CHEMBL5084750

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Cc1nn(CC(F)(F)F)cc1Nc1ncc(C2CC2)c(NCc2ccc(S(N)(=O)=O)cc2)n1

Basic Information

ChEMBL ID CHEMBL5084750
Phase Preclinical
Structure Type MOL
InChI Key MKXAPJAJZRQNMB-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

481.5
MW (Da)
3.42
ALogP
8
HBA
3
HBD
127.8
PSA (Ų)
0.45
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H22F3N7O2S
MW 481.50
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.62

Activity Summary

IC50 3 meas. best 6.83

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase TBK1
CHEMBL5408
IC50 6.83 5.98 149.0 2
Inhibitor of nuclear factor kappa-B kinase subunit epsilon
CHEMBL3529
IC50 5.92 5.92 1199.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34333981 10.1021/acs.jmedchem.1c00440 Serine/threonine-protein kinase TBK1 2
34333981 10.1021/acs.jmedchem.1c00440 Serine/threonine-protein kinase 17A 1
34333981 10.1021/acs.jmedchem.1c00440 MAP/microtubule affinity-regulating kinase 3 1
34333981 10.1021/acs.jmedchem.1c00440 MAP/microtubule affinity-regulating kinase 4 1
34333981 10.1021/acs.jmedchem.1c00440 Inhibitor of nuclear factor kappa-B kinase subunit epsilon 1
34333981 10.1021/acs.jmedchem.1c00440 No relevant target 1
34333981 10.1021/acs.jmedchem.1c00440 ADMET 1

Data from ChEMBL 36 via Core Engine