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Assay Detail

CHEMBL5166839

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

Binding
Inhibition of Eu-W1024 streptavidin-labeled MAGEA4 (unknown origin) expressed in Escherichia coli BL21-(DE3) incubated for 30 to 60 mins by LANCE TR-FRET assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Melanoma-associated antigen 4 (CHEMBL4296022)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Structural Basis of the Selectivity of Potent Cyclic Peptide Inhibitors of MAGE-A4.
Fleming MC, Chiou LF, Tumbale PP, Droby GN, Lim J, Norris-Drouin JL, Williams JG, Pearce KH, Williams RS, Vaziri C, Bowers AA.
J Med Chem (2022) 65 : 7231 -7245
PubMed 35522528 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.88 8.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5199001 1 8.90
CHEMBL5188210 1 8.67
CHEMBL5208958 1 7.97
CHEMBL5182108 1 7.86
CHEMBL5197762 1 7.17
CHEMBL5187977 1 6.99
CHEMBL5175619 1 6.83
CHEMBL5197324 1 6.72
CHEMBL5189065 1 6.06
CHEMBL5174657 1 5.72
CHEMBL5188864 1 5.66
CHEMBL5175748 1 5.65
CHEMBL5202217 1 5.21
CHEMBL5187815 1 -
CHEMBL5174081 1 -
CHEMBL5208599 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5199001 IC50 = 1.26 nM 8.90
CHEMBL5188210 IC50 = 2.15 nM 8.67
CHEMBL5208958 IC50 = 10.6 nM 7.97
CHEMBL5182108 IC50 = 13.9 nM 7.86
CHEMBL5197762 IC50 = 67.5 nM 7.17
CHEMBL5187977 IC50 = 103.1 nM 6.99
CHEMBL5175619 IC50 = 147.55 nM 6.83
CHEMBL5197324 IC50 = 190.14 nM 6.72
CHEMBL5189065 IC50 = 862.2 nM 6.06
CHEMBL5174657 IC50 = 1892.7 nM 5.72
CHEMBL5188864 IC50 = 2211.8 nM 5.66
CHEMBL5175748 IC50 = 2227.95 nM 5.65
CHEMBL5202217 IC50 = 6183.7 nM 5.21
CHEMBL5187815 IC50 < 1.0 nM -
CHEMBL5174081 IC50 < 10000.0 nM -
CHEMBL5208599 IC50 < 10000.0 nM -