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Assay Detail

CHEMBL2150102

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

Functional
Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CCRF-CEM
Confidence 1 — Organism
Curated By Autocuration

Target

CCRF-CEM (CHEMBL382)
Type CELL-LINE
Organism Homo sapiens

Publication

Structure-activity relationship (SAR) study of ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (CXL017) and the potential of the lead against multidrug resistance in cancer treatment.
Aridoss G, Zhou B, Hermanson DL, Bleeker NP, Xing C.
J Med Chem (2012) 55 : 5566 -5581
PubMed 22582991 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.97 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL90555 VINCRISTINE 4.0 1 9.77
CHEMBL803 CYTARABINE 4.0 1 8.22
CHEMBL58 MITOXANTRONE 4.0 1 7.44
CHEMBL53463 DOXORUBICIN 4.0 1 6.96
CHEMBL44657 ETOPOSIDE 4.0 1 6.62
CHEMBL96926 THAPSIGARGIN 1 6.57
CHEMBL376408 ABT 737 1.0 1 6.13
CHEMBL2147958 1 5.83
CHEMBL1915706 1 5.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL90555 VINCRISTINE IC50 = 0.17 nM 9.77
CHEMBL803 CYTARABINE IC50 = 6.0 nM 8.22
CHEMBL58 MITOXANTRONE IC50 = 36.0 nM 7.44
CHEMBL53463 DOXORUBICIN IC50 = 110.0 nM 6.96
CHEMBL44657 ETOPOSIDE IC50 = 240.0 nM 6.62
CHEMBL96926 THAPSIGARGIN IC50 = 270.0 nM 6.57
CHEMBL376408 ABT 737 IC50 = 740.0 nM 6.13
CHEMBL2147958 IC50 = 1470.0 nM 5.83
CHEMBL1915706 IC50 = 7050.0 nM 5.15