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Compound Detail

CHEMBL5423944

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CNC(=O)c1cnc2[nH]ccc2c1N[C@H]1CCN(Cc2ccc(Cl)cn2)[C@@H](C)C1

Basic Information

ChEMBL ID CHEMBL5423944
Phase Preclinical
Structure Type MOL
InChI Key XSKMTIGVIQLGBB-ZFWWWQNUSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

412.9
MW (Da)
3.44
ALogP
5
HBA
3
HBD
85.9
PSA (Ų)
0.60
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H25ClN6O
MW 412.93
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.25

Activity Summary

IC50 4 meas. best 9.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK1
CHEMBL2835
IC50 9.2 9.2 0.6 1
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 8.18 8.18 6.7 1
Tyrosine-protein kinase JAK3
CHEMBL2148
IC50 8.09 8.09 8.1 1
Non-receptor tyrosine-protein kinase TYK2
CHEMBL3553
IC50 8.03 8.03 9.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38031930 10.1021/acs.jmedchem.3c01712 Unchecked 6
38031930 10.1021/acs.jmedchem.3c01712 ADMET 6
38031930 10.1021/acs.jmedchem.3c01712 BaF3 4
38031930 10.1021/acs.jmedchem.3c01712 Tyrosine-protein kinase JAK3 1
38031930 10.1021/acs.jmedchem.3c01712 Non-receptor tyrosine-protein kinase TYK2 1
38031930 10.1021/acs.jmedchem.3c01712 Tyrosine-protein kinase JAK1 1
38031930 10.1021/acs.jmedchem.3c01712 Tyrosine-protein kinase JAK2 1
38031930 10.1021/acs.jmedchem.3c01712 Cytochrome P450 3A4 1
38031930 10.1021/acs.jmedchem.3c01712 Cytochrome P450 2D6 1
38031930 10.1021/acs.jmedchem.3c01712 Cytochrome P450 2C9 1
38031930 10.1021/acs.jmedchem.3c01712 Cytochrome P450 2C19 1
38031930 10.1021/acs.jmedchem.3c01712 Cytochrome P450 1A2 1

Data from ChEMBL 36 via Core Engine