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Compound Detail

CHEMBL5438635

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CNc1cc(Nc2cccn([C@H]3CC[C@@H](OC)CC3)c2=O)nc2c(C(=O)N[C@@H]3CC[C@H]3OC)cnn12

Basic Information

ChEMBL ID CHEMBL5438635
Phase Preclinical
Structure Type MOL
InChI Key RWTRNTPHYFRFAB-YNVMFWSZSA-N
1
Targets
2
Activities
2
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

495.6
MW (Da)
2.71
ALogP
10
HBA
3
HBD
123.8
PSA (Ų)
0.44
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H33N7O4
MW 495.58
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.80

Activity Summary

IC50 1 meas. best 8.02
Kd 1 meas.

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Non-receptor tyrosine-protein kinase TYK2
CHEMBL3553
IC50 8.02 8.02 9.6 1

Pharmacokinetic Data

Parameter Value Units Species
Fu 0.14 - Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
37427891 10.1021/acs.jmedchem.3c00600 Non-receptor tyrosine-protein kinase TYK2 2
37427891 10.1021/acs.jmedchem.3c00600 No relevant target 1
37427891 10.1021/acs.jmedchem.3c00600 ADMET 1

Data from ChEMBL 36 via Core Engine