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Compound Detail

CHEMBL393882

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N=C(N)NCCC[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N1)C(N)=O

Basic Information

ChEMBL ID CHEMBL393882
Phase Preclinical
Structure Type BOTH
InChI Key DGQKRQOCJFODHN-OIHVMPBRSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

2037.5
MW (Da)

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C90H141N33O18S2
MW 2037.47

Activity Summary

IC50 1 meas. best 9.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C-X-C chemokine receptor type 4
CHEMBL2107
IC50 9.22 9.22 0.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
C-X-C chemokine receptor type 4 IC50 = 0.6 nM 9.22 Inhibition of CXCR4 in MDA-MB-231 cells 17958344

Literature References

PubMed DOI Target Context # Activities
21105715 10.1021/jm100786g Mus musculus 4
17958344 10.1021/jm070679i C-X-C chemokine receptor type 4 1
17958344 10.1021/jm070679i MDA-MB-231 1
17958344 10.1021/jm070679i Unchecked 1
21105715 10.1021/jm100786g NON-PROTEIN TARGET 1
21105715 10.1021/jm100786g MDA-MB-231 1

Data from ChEMBL 36 via Core Engine