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Compound Detail

CHEMBL5092577

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CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3nc(Nc4ccc(C(=O)NC5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)cc4)nc4[nH]ccc34)cn2)C1

Basic Information

ChEMBL ID CHEMBL5092577
Phase Preclinical
Structure Type MOL
InChI Key QENXNFNQQOSOIZ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

844.9
MW (Da)
2.64
ALogP
14
HBA
4
HBD
248.5
PSA (Ų)
0.14
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C41H40N12O7S
MW 844.91
Aromatic Rings 5
Heavy Atoms 61
NP-Likeness -1.10

Activity Summary

IC50 1 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein cereblon
CHEMBL3763008
IC50 7.7 7.7 20.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein cereblon IC50 = 20.2 nM 7.7 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 Unchecked 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