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Compound Detail

CHEMBL5416354

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C=CC(=O)Nc1cc(CNc2nc(Nc3ccc(N4CCN(C)CC4)c(OC)c3)c(C(N)=O)c3nccn23)ccc1Cl

Basic Information

ChEMBL ID CHEMBL5416354
Phase Preclinical
Structure Type MOL
InChI Key AYZVUGQJVYMELX-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

590.1
MW (Da)
3.72
ALogP
10
HBA
4
HBD
142.2
PSA (Ų)
0.20
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H32ClN9O3
MW 590.09
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -1.43

Activity Summary

IC50 2 meas. best 8.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase ZAP-70
CHEMBL2803
IC50 8.34 8.34 4.6 1
Tyrosine-protein kinase SYK
CHEMBL2599
IC50 6.27 6.27 532.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
37594408 10.1021/acs.jmedchem.3c00606 Tyrosine-protein kinase SYK 2
37594408 10.1021/acs.jmedchem.3c00606 Tyrosine-protein kinase ZAP-70 2
37594408 10.1021/acs.jmedchem.3c00606 Splenocyte 1

Data from ChEMBL 36 via Core Engine