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Assay Detail

CHEMBL3367171

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

Binding
Inhibition of AP-1-mediated transcriptional activation in human Jurkat cells by luciferase reporter gene assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Transcription factor Jun (CHEMBL4977)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Small molecule inhibitors targeting activator protein 1 (AP-1).
Ye N, Ding Y, Wild C, Shen Q, Zhou J.
J Med Chem (2014) 57 : 6930 -6948
PubMed 24831826 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 6.33 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL337665 1 8.52
CHEMBL129857 AS-602868 1.0 1 8.10
CHEMBL43549 1 7.70
CHEMBL132495 1 7.70
CHEMBL85822 1 7.46
CHEMBL86615 1 7.35
CHEMBL336546 1 7.30
CHEMBL315804 1 7.01
CHEMBL3341912 1 7.00
CHEMBL42952 1 7.00
CHEMBL131006 1 7.00
CHEMBL340779 1 6.70
CHEMBL87274 1 6.68
CHEMBL87433 1 6.52
CHEMBL423150 1 6.40
CHEMBL83026 1 6.40
CHEMBL3341901 1 6.30
CHEMBL3341914 1 6.12
CHEMBL3341913 1 6.08
CHEMBL42719 1 6.00
CHEMBL338934 1 5.77
CHEMBL3341911 1 5.72
CHEMBL87572 1 5.70
CHEMBL340410 1 5.40
CHEMBL88100 1 5.36
CHEMBL3341908 1 5.21
CHEMBL3341909 1 5.07
CHEMBL3341906 1 5.03
CHEMBL3341907 1 5.03
CHEMBL128708 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL337665 IC50 = 3.0 nM 8.52
CHEMBL129857 AS-602868 IC50 = 8.0 nM 8.10
CHEMBL132495 IC50 = 20.0 nM 7.70
CHEMBL43549 IC50 = 20.0 nM 7.70
CHEMBL85822 IC50 = 35.0 nM 7.46
CHEMBL86615 IC50 = 45.0 nM 7.35
CHEMBL336546 IC50 = 50.0 nM 7.30
CHEMBL315804 IC50 = 98.0 nM 7.01
CHEMBL131006 IC50 = 100.0 nM 7.00
CHEMBL42952 IC50 = 100.0 nM 7.00
CHEMBL3341912 IC50 = 100.0 nM 7.00
CHEMBL340779 IC50 = 200.0 nM 6.70
CHEMBL87274 IC50 = 210.0 nM 6.68
CHEMBL87433 IC50 = 300.0 nM 6.52
CHEMBL83026 IC50 = 400.0 nM 6.40
CHEMBL423150 IC50 = 400.0 nM 6.40
CHEMBL3341901 IC50 = 500.0 nM 6.30
CHEMBL3341914 IC50 = 760.0 nM 6.12
CHEMBL3341913 IC50 = 830.0 nM 6.08
CHEMBL42719 IC50 = 1000.0 nM 6.00
CHEMBL338934 IC50 = 1700.0 nM 5.77
CHEMBL3341911 IC50 = 1900.0 nM 5.72
CHEMBL87572 IC50 = 2000.0 nM 5.70
CHEMBL340410 IC50 = 4000.0 nM 5.40
CHEMBL88100 IC50 = 4400.0 nM 5.36
CHEMBL3341908 IC50 = 6100.0 nM 5.21
CHEMBL3341909 IC50 = 8500.0 nM 5.07
CHEMBL3341907 IC50 = 9400.0 nM 5.03
CHEMBL3341906 IC50 = 9400.0 nM 5.03
CHEMBL128708 IC50 = 10000.0 nM 5.00
CHEMBL3341905 IC50 = 10000.0 nM 5.00
CHEMBL3341910 IC50 = 10000.0 nM 5.00
CHEMBL132457 IC50 > 30000.0 nM -
CHEMBL3341903 IC50 > 10000.0 nM -
CHEMBL3341902 IC50 > 10000.0 nM -
CHEMBL128808 IC50 > 10000.0 nM -
CHEMBL128314 IC50 > 10000.0 nM -