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Compound Detail

CHEMBL4476261

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CNC(=O)c1cnc(NC(=O)C2CC2)cc1Nc1cccc(-c2ncn(C)n2)c1OC

Basic Information

ChEMBL ID CHEMBL4476261
Phase Preclinical
Structure Type MOL
InChI Key FYXUGQDHTWRPDY-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

421.5
MW (Da)
2.34
ALogP
8
HBA
3
HBD
123.1
PSA (Ų)
0.53
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23N7O3
MW 421.46
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.35

Activity Summary

IC50 4 meas. best 9.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Non-receptor tyrosine-protein kinase TYK2
CHEMBL3553
IC50 9.15 8.475 0.7 2
JAK1/TYK2
CHEMBL3301391
IC50 7.85 7.85 14.0 1
Non-receptor tyrosine-protein kinase TYK2
CHEMBL2321619
IC50 6.48 6.48 330.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31318208 10.1021/acs.jmedchem.9b00444 Non-receptor tyrosine-protein kinase TYK2 2
31318208 10.1021/acs.jmedchem.9b00444 ADMET 2
31318208 10.1021/acs.jmedchem.9b00444 JAK1/TYK2 1
31318208 10.1021/acs.jmedchem.9b00444 Voltage-gated inwardly rectifying potassium channel KCNH2 1
38781921 10.1016/j.ejmech.2024.116364 Non-receptor tyrosine-protein kinase TYK2 1

Data from ChEMBL 36 via Core Engine