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Compound Detail

CHEMBL5439922

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C[C@@H]1CCC2[C@@H](C)[C@@H](OCCN(CCO[C@H]3O[C@@H]4O[C@@]5(C)CCC6[C@H](C)CCC([C@H]3C)[C@]64OO5)C(=O)CCCCCCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)O[C@@H]3O[C@@]4(C)CCC1[C@@]23OO4

Basic Information

ChEMBL ID CHEMBL5439922
Phase Preclinical
Structure Type MOL
InChI Key ZLJLKXURBBWTFW-RJHWUJBZSA-N
4
Targets
4
Activities
2
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

1035.2
MW (Da)

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C55H78N4O15
MW 1035.24

Activity Summary

IC50 3 meas. best 7.3
Kd 1 meas. best 5.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
RS4-11
CHEMBL2366159
IC50 7.3 7.3 50.6 1
RPMI-8226
CHEMBL614882
IC50 6.63 6.63 235.3 1
U-266
CHEMBL2366315
IC50 6.46 6.46 342.8 1
PCNA-associated factor
CHEMBL5574
Kd 5.21 5.21 6100.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 24.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
37552639 10.1021/acs.jmedchem.3c00824 Protein cereblon/PCNA-associated factor 13
37552639 10.1021/acs.jmedchem.3c00824 RS4-11 10
37552639 10.1021/acs.jmedchem.3c00824 ADMET 10
37552639 10.1021/acs.jmedchem.3c00824 PCNA-associated factor 2
37552639 10.1021/acs.jmedchem.3c00824 RPMI-8226 1
37552639 10.1021/acs.jmedchem.3c00824 U-266 1

Data from ChEMBL 36 via Core Engine