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Compound Detail

CHEMBL4082676

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CC(C)(C)CNC(=O)C[C@H](NC(=O)C1CCN(C(=O)c2ccc(F)cc2)CC1)C(=O)N[C@@H](CCc1ccccc1)C(=O)NCc1ccccc1Cl

Basic Information

ChEMBL ID CHEMBL4082676
Phase Preclinical
Structure Type MOL
InChI Key PJHIACOTCUHJGN-LQJZCPKCSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

720.3
MW (Da)
4.80
ALogP
5
HBA
4
HBD
136.7
PSA (Ų)
0.19
QED
1
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C39H47ClFN5O5
MW 720.29
Aromatic Rings 3
Heavy Atoms 51
NP-Likeness -1.19

Activity Summary

IC50 3 meas. best 8.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proteasome Macropain subunit MB1
CHEMBL4662
IC50 8.59 8.59 2.6 1
RPMI-8226
CHEMBL614882
IC50 7.64 7.64 22.7 1
MM1.S
CHEMBL4296471
IC50 7.5 7.5 31.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28027531 10.1016/j.ejmech.2016.12.034 RPMI-8226 1
28027531 10.1016/j.ejmech.2016.12.034 Proteasome Macropain subunit MB1 1
28027531 10.1016/j.ejmech.2016.12.034 MM1.S 1

Data from ChEMBL 36 via Core Engine