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Assay Detail

CHEMBL5099172

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

Functional
Reversal of 5-FU resistance in human HCT-116 cells overexpressing DPD assessed as reduction in cell viability incubated for 48 hrs in presence of 5-FU by MTT assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT-116
Confidence 1 — Organism
Curated By Autocuration

Target

HCT-116 (CHEMBL394)
Type CELL-LINE
Organism Homo sapiens

Publication

Rational Design, Synthesis, and Biological Evaluation of Novel S1PR2 Antagonists for Reversing 5-FU-Resistance in Colorectal Cancer.
Luo D, Liu X, Jiang L, Guo Z, Lv Y, Tian X, Wang X, Cui S, Wan S, Qu X, Xu X, Li X.
J Med Chem (2022) 65 : 14553 -14577
PubMed 36269639 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.39 5.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3401388 1 5.67
CHEMBL5181599 1 5.58
CHEMBL5206026 1 5.54
CHEMBL5193759 1 5.53
CHEMBL5172220 1 5.50
CHEMBL5206290 1 5.40
CHEMBL5208524 1 5.19
CHEMBL3759434 1 4.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3401388 IC50 = 2160.0 nM 5.67
CHEMBL5181599 IC50 = 2650.0 nM 5.58
CHEMBL5206026 IC50 = 2860.0 nM 5.54
CHEMBL5193759 IC50 = 2930.0 nM 5.53
CHEMBL5172220 IC50 = 3160.0 nM 5.50
CHEMBL5206290 IC50 = 3960.0 nM 5.40
CHEMBL5208524 IC50 = 6420.0 nM 5.19
CHEMBL3759434 IC50 = 18360.0 nM 4.74