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Assay Detail

CHEMBL5057382

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

Functional
Reversal of resistance to paclitaxel-induced cytotoxicity in human SW-620/AD300 cells assessed as reduction in paclitaxel IC50 at 1 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 4.23 +/- 0.50 uM)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SW-620
Confidence 1 — Organism
Curated By Autocuration

Target

SW-620 (CHEMBL612262)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of the Triazolo[1,5-<i>a</i>]Pyrimidine-Based Derivative WS-898 as a Highly Efficacious and Orally Bioavailable ABCB1 Inhibitor Capable of Overcoming Multidrug Resistance.
Wang S, Wang SQ, Teng QX, Lei ZN, Chen ZS, Chen XB, Liu HM, Yu B.
J Med Chem (2021) 64 : 16187 -16204
PubMed 34723530 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.00 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5070340 1 7.55
CHEMBL4776099 1 7.24
CHEMBL4091439 1 7.12
CHEMBL4781900 1 6.96
CHEMBL5085203 1 6.92
CHEMBL5084491 1 6.62
CHEMBL5086344 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5070340 IC50 = 28.15 nM 7.55
CHEMBL4776099 IC50 = 58.0 nM 7.24
CHEMBL4091439 IC50 = 75.0 nM 7.12
CHEMBL4781900 IC50 = 110.0 nM 6.96
CHEMBL5085203 IC50 = 120.0 nM 6.92
CHEMBL5084491 IC50 = 240.0 nM 6.62
CHEMBL5086344 IC50 = 260.0 nM 6.58