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Assay Detail

CHEMBL2434703

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

Binding
Competitive binding affinity to Stat3 SH2 domain (unknown origin) using 5-FAM-GpYLPQTV-NH2 as probe assessed as phosphopetide complex formation after 30 mins by fluorescence polarization assay
75
Total Activities
75
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

Signal transducer and activator of transcription 3 (CHEMBL4026)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibiting aberrant signal transducer and activator of transcription protein activation with tetrapodal, small molecule Src homology 2 domain binders: promising agents against multiple myeloma.
Page BD, Croucher DC, Li ZH, Haftchenary S, Jimenez-Zepeda VH, Atkinson J, Spagnuolo PA, Wong YL, Colaguori R, Lewis AM, Schimmer AD, Trudel S, Gunning PT.
J Med Chem (2013) 56 : 7190 -7200
PubMed 23968501 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 75 4.86 5.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2431993 1 5.55
CHEMBL2431942 1 5.30
CHEMBL2431970 1 5.30
CHEMBL2431991 1 5.28
CHEMBL2431964 1 5.22
CHEMBL2431965 1 5.21
CHEMBL2431966 1 5.14
CHEMBL2431945 1 5.12
CHEMBL2431962 1 5.12
CHEMBL2431967 1 5.10
CHEMBL2431941 1 5.09
CHEMBL2431980 1 5.07
CHEMBL2431990 1 5.06
CHEMBL2431961 1 5.05
CHEMBL2431995 1 5.04
CHEMBL2431931 1 5.03
CHEMBL2431956 1 5.02
CHEMBL2431944 1 5.02
CHEMBL2431969 1 5.00
CHEMBL2431926 1 4.99
CHEMBL2431994 1 4.99
CHEMBL2431960 1 4.97
CHEMBL2431923 1 4.96
CHEMBL2431971 1 4.96
CHEMBL2431943 1 4.96
CHEMBL2431935 1 4.96
CHEMBL2431929 1 4.94
CHEMBL2431947 1 4.94
CHEMBL2431968 1 4.93
CHEMBL2431952 1 4.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2431993 IC50 = 2800.0 nM 5.55
CHEMBL2431942 IC50 = 5000.0 nM 5.30
CHEMBL2431970 IC50 = 5000.0 nM 5.30
CHEMBL2431991 IC50 = 5200.0 nM 5.28
CHEMBL2431964 IC50 = 6000.0 nM 5.22
CHEMBL2431965 IC50 = 6200.0 nM 5.21
CHEMBL2431966 IC50 = 7200.0 nM 5.14
CHEMBL2431945 IC50 = 7600.0 nM 5.12
CHEMBL2431962 IC50 = 7600.0 nM 5.12
CHEMBL2431967 IC50 = 8000.0 nM 5.10
CHEMBL2431941 IC50 = 8100.0 nM 5.09
CHEMBL2431980 IC50 = 8600.0 nM 5.07
CHEMBL2431990 IC50 = 8800.0 nM 5.06
CHEMBL2431961 IC50 = 9000.0 nM 5.05
CHEMBL2431995 IC50 = 9200.0 nM 5.04
CHEMBL2431931 IC50 = 9400.0 nM 5.03
CHEMBL2431956 IC50 = 9600.0 nM 5.02
CHEMBL2431944 IC50 = 9600.0 nM 5.02
CHEMBL2431969 IC50 = 10000.0 nM 5.00
CHEMBL2431926 IC50 = 10200.0 nM 4.99
CHEMBL2431994 IC50 = 10200.0 nM 4.99
CHEMBL2431960 IC50 = 10600.0 nM 4.97
CHEMBL2431935 IC50 = 11000.0 nM 4.96
CHEMBL2431943 IC50 = 11000.0 nM 4.96
CHEMBL2431923 IC50 = 11000.0 nM 4.96
CHEMBL2431971 IC50 = 11000.0 nM 4.96
CHEMBL2431929 IC50 = 11400.0 nM 4.94
CHEMBL2431947 IC50 = 11600.0 nM 4.94
CHEMBL2431968 IC50 = 11800.0 nM 4.93
CHEMBL2431952 IC50 = 11800.0 nM 4.93
CHEMBL2431932 IC50 = 12400.0 nM 4.91
CHEMBL2431979 IC50 = 12400.0 nM 4.91
CHEMBL2431973 IC50 = 12400.0 nM 4.91
CHEMBL2431955 IC50 = 12800.0 nM 4.89
CHEMBL2431925 IC50 = 13800.0 nM 4.86
CHEMBL2431953 IC50 = 14600.0 nM 4.84
CHEMBL2431989 IC50 = 14400.0 nM 4.84
CHEMBL2431951 IC50 = 14400.0 nM 4.84
CHEMBL2431954 IC50 = 14400.0 nM 4.84
CHEMBL2431939 IC50 = 15400.0 nM 4.81
CHEMBL2431963 IC50 = 15800.0 nM 4.80
CHEMBL2023989 IC50 = 15800.0 nM 4.80
CHEMBL2431934 IC50 = 16600.0 nM 4.78
CHEMBL2431986 IC50 = 17000.0 nM 4.77
CHEMBL2431937 IC50 = 17400.0 nM 4.76
CHEMBL2431933 IC50 = 17600.0 nM 4.75
CHEMBL2431927 IC50 = 17800.0 nM 4.75
CHEMBL2431922 IC50 = 17600.0 nM 4.75
CHEMBL2431959 IC50 = 17800.0 nM 4.75
CHEMBL2431985 IC50 = 17800.0 nM 4.75