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Compound Detail

CHEMBL5273652

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CN(C)C(=O)c1cn(C2CCCC2)c2cnc(Nc3ccc(N4CCN(c5cn(CCCCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)nn5)CC4)cn3)nc12

Basic Information

ChEMBL ID CHEMBL5273652
Phase Preclinical
Structure Type MOL
InChI Key FCURMICREJRIDK-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

843.0
MW (Da)
3.99
ALogP
16
HBA
3
HBD
208.7
PSA (Ų)
0.11
QED
2
Ro5 Violations
14
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C43H50N14O5
MW 842.97
Aromatic Rings 5
Heavy Atoms 62
NP-Likeness -1.22

Activity Summary

EC50 1 meas. best 7.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein cereblon/Cyclin-dependent kinase 4
CHEMBL4523686
EC50 7.01 7.01 97.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein cereblon/Cyclin-dependent kinase 4 EC50 = 97.0 nM 7.01 Protac activity at CRBN/CDK4 in human MDA-MB-231 cells 36274273

Literature References

PubMed DOI Target Context # Activities
36274273 10.1016/j.ejmech.2022.114838 Protein cereblon/Cyclin-dependent kinase 4 1

Data from ChEMBL 36 via Core Engine