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Compound Detail

CHEMBL4777817

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Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCNC(=O)CCC(=O)N2CCN([C@H]3CC[C@@H](Nc4ncnn5ccc(C(C)C)c45)CC3)CC2)C(C)(C)C)cc1

Basic Information

ChEMBL ID CHEMBL4777817
Phase Preclinical
Structure Type MOL
InChI Key PDSUGWAIWCZKFS-SRCMZFQMSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

982.3
MW (Da)
5.81
ALogP
13
HBA
5
HBD
206.5
PSA (Ų)
0.07
QED
3
Ro5 Violations
20
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C52H75N11O6S
MW 982.31
Aromatic Rings 4
Heavy Atoms 70
NP-Likeness -0.81

Activity Summary

IC50 1 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Interleukin-1 receptor-associated kinase 3
CHEMBL5081
IC50 8.22 8.22 6.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32803978 10.1021/acs.jmedchem.0c01125 von Hippel-Lindau disease tumor suppressor/IRAK3 2
32803978 10.1021/acs.jmedchem.0c01125 Unchecked 1
32803978 10.1021/acs.jmedchem.0c01125 Interleukin-1 receptor-associated kinase 3 1
32803978 10.1021/acs.jmedchem.0c01125 Interleukin-1 receptor-associated kinase 4 1

Data from ChEMBL 36 via Core Engine