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Assay Detail

CHEMBL2150100

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

Functional
Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay
54
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HL-60
Confidence 1 — Organism
Curated By Autocuration

Target

HL-60 (CHEMBL383)
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 54 5.35 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL96926 THAPSIGARGIN 1 8.15
CHEMBL58 MITOXANTRONE 4.0 1 7.80
CHEMBL53463 DOXORUBICIN 4.0 1 7.40
CHEMBL803 CYTARABINE 4.0 1 7.31
CHEMBL90555 VINCRISTINE 4.0 1 7.22
CHEMBL44657 ETOPOSIDE 4.0 1 6.96
CHEMBL2147958 1 6.21
CHEMBL2147954 1 6.20
CHEMBL376408 ABT 737 1.0 1 6.12
CHEMBL2147961 1 6.06
CHEMBL2147890 1 5.91
CHEMBL1819010 1 5.82
CHEMBL2147967 1 5.79
CHEMBL2147964 1 5.73
CHEMBL2147871 1 5.62
CHEMBL2147968 1 5.61
CHEMBL2147969 1 5.59
CHEMBL2147889 1 5.47
CHEMBL1819011 1 5.33
CHEMBL1819009 1 5.33
CHEMBL2147965 1 5.28
CHEMBL2147966 1 5.27
CHEMBL1915706 1 5.17
CHEMBL1819012 1 5.17
CHEMBL2147960 1 5.15
CHEMBL2147971 1 5.14
CHEMBL2147959 1 5.13
CHEMBL1818900 1 5.12
CHEMBL2147885 1 4.99
CHEMBL2147887 1 4.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL96926 THAPSIGARGIN IC50 = 7.0 nM 8.15
CHEMBL58 MITOXANTRONE IC50 = 16.0 nM 7.80
CHEMBL53463 DOXORUBICIN IC50 = 40.0 nM 7.40
CHEMBL803 CYTARABINE IC50 = 49.0 nM 7.31
CHEMBL90555 VINCRISTINE IC50 = 60.0 nM 7.22
CHEMBL44657 ETOPOSIDE IC50 = 110.0 nM 6.96
CHEMBL2147958 IC50 = 610.0 nM 6.21
CHEMBL2147954 IC50 = 630.0 nM 6.20
CHEMBL376408 ABT 737 IC50 = 760.0 nM 6.12
CHEMBL2147961 IC50 = 880.0 nM 6.06
CHEMBL2147890 IC50 = 1240.0 nM 5.91
CHEMBL1819010 IC50 = 1500.0 nM 5.82
CHEMBL2147967 IC50 = 1620.0 nM 5.79
CHEMBL2147964 IC50 = 1860.0 nM 5.73
CHEMBL2147871 IC50 = 2420.0 nM 5.62
CHEMBL2147968 IC50 = 2450.0 nM 5.61
CHEMBL2147969 IC50 = 2560.0 nM 5.59
CHEMBL2147889 IC50 = 3400.0 nM 5.47
CHEMBL1819011 IC50 = 4700.0 nM 5.33
CHEMBL1819009 IC50 = 4700.0 nM 5.33
CHEMBL2147965 IC50 = 5300.0 nM 5.28
CHEMBL2147966 IC50 = 5400.0 nM 5.27
CHEMBL1915706 IC50 = 6800.0 nM 5.17
CHEMBL1819012 IC50 = 6700.0 nM 5.17
CHEMBL2147960 IC50 = 7130.0 nM 5.15
CHEMBL2147971 IC50 = 7270.0 nM 5.14
CHEMBL2147959 IC50 = 7450.0 nM 5.13
CHEMBL1818900 IC50 = 7600.0 nM 5.12
CHEMBL2147885 IC50 = 10200.0 nM 4.99
CHEMBL2147887 IC50 = 10200.0 nM 4.99
CHEMBL2147957 IC50 = 10500.0 nM 4.98
CHEMBL2147872 IC50 = 10800.0 nM 4.97
CHEMBL561602 IC50 = 10700.0 nM 4.97
CHEMBL2147962 IC50 = 12000.0 nM 4.92
CHEMBL2147963 IC50 = 17200.0 nM 4.76
CHEMBL2147874 IC50 = 19600.0 nM 4.71
CHEMBL2147888 IC50 = 20200.0 nM 4.70
CHEMBL2147884 IC50 = 21500.0 nM 4.67
CHEMBL2147956 IC50 = 22300.0 nM 4.65
CHEMBL1819008 IC50 = 32000.0 nM 4.50
CHEMBL2147970 IC50 = 33000.0 nM 4.48
CHEMBL2147880 IC50 = 35900.0 nM 4.45
CHEMBL2147886 IC50 = 37900.0 nM 4.42
CHEMBL2147955 IC50 = 43900.0 nM 4.36
CHEMBL2147878 IC50 = 72100.0 nM 4.14
CHEMBL2147876 IC50 = 73000.0 nM 4.14
CHEMBL2147879 IC50 = 76600.0 nM 4.12
CHEMBL2147877 IC50 = 76400.0 nM 4.12
CHEMBL2147883 IC50 = 76900.0 nM 4.11
CHEMBL560141 IC50 = 91000.0 nM 4.04