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Compound Detail

CHEMBL5074539

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CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3nc(Nc4ccc(C(=O)NCCCN5CCC6(CC5)CCN(c5ccc(C7CCC(=O)NC7=O)cc5)CC6)cc4)nc4[nH]ccc34)cn2)C1

Basic Information

ChEMBL ID CHEMBL5074539
Phase Preclinical
Structure Type MOL
InChI Key NTHVTKVZITWROX-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

887.1
MW (Da)
4.86
ALogP
13
HBA
4
HBD
214.3
PSA (Ų)
0.09
QED
2
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C46H54N12O5S
MW 887.08
Aromatic Rings 5
Heavy Atoms 64
NP-Likeness -1.00

Activity Summary

IC50 1 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein cereblon
CHEMBL3763008
IC50 7.82 7.82 15.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein cereblon IC50 = 15.0 nM 7.82 Binding affinity to CRBN (unknown origin) measured by Fluorescent Polarization a... 35300081

Literature References

PubMed DOI Target Context # Activities
35300081 10.1021/acsmedchemlett.1c00650 Protein cereblon/Tyrosine-protein kinase JAK2 1
35300081 10.1021/acsmedchemlett.1c00650 Protein cereblon/GSPT1 1
35300081 10.1021/acsmedchemlett.1c00650 Protein cereblon 1

Data from ChEMBL 36 via Core Engine