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Assay Detail

CHEMBL1810396

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

Functional
Cytotoxicity against multidrug-resistant human A2780AD cells overexpressing p-gp after 48 hrs by MTT assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A2780 ADR
Confidence 1 — Organism
Curated By Autocuration

Publication

Effects of C7 substitutions in a high affinity microtubule-binding taxane on antitumor activity and drug transport.
Xiao X, Wu J, Trigili C, Chen H, Chu JW, Zhao Y, Lu P, Sheng L, Li Y, Sharom FJ, Barasoain I, Diaz JF, Fang WS.
Bioorg Med Chem Lett (2011) 21 : 4852 -4856
PubMed 21764308 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.23 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1809080 1 7.85
CHEMBL1809086 1 6.77
CHEMBL1809081 1 6.53
CHEMBL1809084 1 6.15
CHEMBL1809083 1 6.06
CHEMBL1809088 1 6.02
CHEMBL1809085 1 5.89
CHEMBL1809087 1 5.85
CHEMBL428647 PACLITAXEL 4.0 1 5.72
CHEMBL1809082 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1809080 IC50 = 14.0 nM 7.85
CHEMBL1809086 IC50 = 170.0 nM 6.77
CHEMBL1809081 IC50 = 293.0 nM 6.53
CHEMBL1809084 IC50 = 710.0 nM 6.15
CHEMBL1809083 IC50 = 875.0 nM 6.06
CHEMBL1809088 IC50 = 950.0 nM 6.02
CHEMBL1809085 IC50 = 1300.0 nM 5.89
CHEMBL1809087 IC50 = 1400.0 nM 5.85
CHEMBL428647 PACLITAXEL IC50 = 1900.0 nM 5.72
CHEMBL1809082 IC50 = 3200.0 nM 5.50