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Assay Detail

CHEMBL914595

Review assay metadata, readout intent, target linkage, and publication context from the same page.

ADMET
Cytotoxicity against human KB cells after 72 hrs
27
Total Activities
27
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type KB
Confidence 1 — Organism
Curated By Autocuration

Target

KB (CHEMBL398)
Type CELL-LINE
Organism Homo sapiens

Publication

Novel C2-C3' N-peptide linked macrocyclic taxoids. Part 2: synthesis and biological activities of docetaxel analogues with a peptide side chain at C2 and their macrocyclic derivatives.
Larroque AL, Dubois J, Thoret S, Aubert G, Chiaroni A, Guéritte F, Guénard D.
Bioorg Med Chem (2007) 15 : 563 -574
PubMed 17064914 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.88 10.00
Activity 11 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3545252 DOCETAXEL 4.0 1 10.00
CHEMBL426016 1 8.40
CHEMBL224082 1 7.30
CHEMBL375041 1 7.05
CHEMBL376131 1 7.05
CHEMBL224542 1 7.00
CHEMBL375887 1 6.17
CHEMBL224592 1 5.98
CHEMBL388563 1 5.96
CHEMBL388562 1 5.40
CHEMBL388306 1 5.35
CHEMBL426186 1 -
CHEMBL225259 1 -
CHEMBL448780 1 -
CHEMBL387904 1 -
CHEMBL390328 1 -
CHEMBL375713 1 -
CHEMBL413716 1 -
CHEMBL227409 1 -
CHEMBL389420 1 -
CHEMBL414121 1 -
CHEMBL390836 1 -
CHEMBL226922 1 -
CHEMBL376361 1 -
CHEMBL226708 1 -
CHEMBL228101 1 -
CHEMBL376362 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3545252 DOCETAXEL IC50 = 0.1 nM 10.00
CHEMBL426016 IC50 = 4.0 nM 8.40
CHEMBL224082 IC50 = 50.0 nM 7.30
CHEMBL375041 IC50 = 90.0 nM 7.05
CHEMBL376131 IC50 = 90.0 nM 7.05
CHEMBL224542 IC50 = 100.0 nM 7.00
CHEMBL375887 IC50 = 670.0 nM 6.17
CHEMBL224592 IC50 = 1050.0 nM 5.98
CHEMBL388563 IC50 = 1100.0 nM 5.96
CHEMBL388562 IC50 = 4000.0 nM 5.40
CHEMBL388306 IC50 = 4500.0 nM 5.35
CHEMBL426186 IC50 > 10000.0 nM -
CHEMBL225259 IC50 > 10000.0 nM -
CHEMBL448780 IC50 > 10000.0 nM -
CHEMBL387904 IC50 > 10000.0 nM -
CHEMBL390328 IC50 > 10000.0 nM -
CHEMBL375713 Activity - -
CHEMBL413716 Activity - -
CHEMBL227409 Activity - -
CHEMBL389420 Activity - -
CHEMBL414121 Activity - -
CHEMBL390836 Activity - -
CHEMBL226922 Activity - -
CHEMBL376361 Activity - -
CHEMBL226708 Activity - -
CHEMBL228101 Activity - -
CHEMBL376362 Activity - -