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Assay Detail

CHEMBL704798

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Functional
Inhibition of AP-1 and NF-kB-mediated transcriptional activation in Jurkat cells
ChEMBL ↗
57
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Jurkat
Confidence 1 — Organism
Curated By Expert

Target

Jurkat (CHEMBL397) ↗
Type CELL-LINE
Organism Homo sapiens

Publication

Structure-activity relationship studies of ethyl 2-[(3-methyl-2,5-dioxo(3-pyrrolinyl))amino]-4-(trifluoromethyl)pyrimidine-5-carboxylate: an inhibitor of AP-1 and NF-kappaB mediated gene expression.
Palanki MS, Gayo-Fung LM, Shevlin GI, Erdman P, Sato M, Goldman M, Ransone LJ, Spooner C.
Bioorg Med Chem Lett (2002) 12 : 2573 -2577
PubMed 12182863 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 57 6.00 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85822 — — 1 7.46
CHEMBL86615 — — 1 7.35
CHEMBL84791 — — 1 7.30
CHEMBL87876 — — 1 7.03
CHEMBL315804 — — 1 7.01
CHEMBL85908 — — 1 6.92
CHEMBL85553 — — 1 6.92
CHEMBL87338 — — 1 6.89
CHEMBL312978 — — 1 6.85
CHEMBL82972 — — 1 6.70
CHEMBL315069 — — 1 6.70
CHEMBL87274 — — 1 6.68
CHEMBL87433 — — 1 6.52
CHEMBL430646 — — 2 6.46
CHEMBL315336 — — 1 6.46
CHEMBL85293 — — 1 6.42
CHEMBL83026 — — 1 6.40
CHEMBL423679 — — 1 6.39
CHEMBL87457 — — 1 6.39
CHEMBL87877 — — 1 6.37
CHEMBL419856 — — 1 6.35
CHEMBL314158 — — 1 6.35
CHEMBL315941 — — 1 6.28
CHEMBL315145 — — 1 6.23
CHEMBL86332 — — 1 6.20
CHEMBL83024 — — 1 6.19
CHEMBL418938 — — 1 6.12
CHEMBL316427 — — 1 6.10
CHEMBL432946 — — 1 6.08
CHEMBL314316 — — 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85822 — IC50 = 35.0 nM 7.46
CHEMBL86615 — IC50 = 45.0 nM 7.35
CHEMBL84791 — IC50 = 50.0 nM 7.30
CHEMBL87876 — IC50 = 94.0 nM 7.03
CHEMBL315804 — IC50 = 98.0 nM 7.01
CHEMBL85908 — IC50 = 120.0 nM 6.92
CHEMBL85553 — IC50 = 120.0 nM 6.92
CHEMBL87338 — IC50 = 130.0 nM 6.89
CHEMBL312978 — IC50 = 140.0 nM 6.85
CHEMBL315069 — IC50 = 200.0 nM 6.70
CHEMBL82972 — IC50 = 200.0 nM 6.70
CHEMBL87274 — IC50 = 210.0 nM 6.68
CHEMBL87433 — IC50 = 300.0 nM 6.52
CHEMBL315336 — IC50 = 350.0 nM 6.46
CHEMBL430646 — IC50 = 350.0 nM 6.46
CHEMBL85293 — IC50 = 380.0 nM 6.42
CHEMBL83026 — IC50 = 400.0 nM 6.40
CHEMBL87457 — IC50 = 410.0 nM 6.39
CHEMBL423679 — IC50 = 410.0 nM 6.39
CHEMBL87877 — IC50 = 430.0 nM 6.37
CHEMBL430646 — IC50 = 450.0 nM 6.35
CHEMBL419856 — IC50 = 450.0 nM 6.35
CHEMBL314158 — IC50 = 450.0 nM 6.35
CHEMBL315941 — IC50 = 520.0 nM 6.28
CHEMBL315145 — IC50 = 590.0 nM 6.23
CHEMBL86332 — IC50 = 630.0 nM 6.20
CHEMBL83024 — IC50 = 650.0 nM 6.19
CHEMBL418938 — IC50 = 760.0 nM 6.12
CHEMBL316427 — IC50 = 800.0 nM 6.10
CHEMBL432946 — IC50 = 830.0 nM 6.08
CHEMBL314316 — IC50 = 830.0 nM 6.08
CHEMBL87789 — IC50 = 1000.0 nM 6.00
CHEMBL87795 — IC50 = 1100.0 nM 5.96
CHEMBL85285 — IC50 = 1200.0 nM 5.92
CHEMBL87269 — IC50 = 1500.0 nM 5.82
CHEMBL87359 — IC50 = 1600.0 nM 5.80
CHEMBL313824 — IC50 = 1700.0 nM 5.77
CHEMBL315919 — IC50 = 1900.0 nM 5.72
CHEMBL87572 — IC50 = 2000.0 nM 5.70
CHEMBL87744 — IC50 = 2200.0 nM 5.66
CHEMBL84869 — IC50 = 2800.0 nM 5.55
CHEMBL316150 — IC50 = 3700.0 nM 5.43
CHEMBL87467 — IC50 = 3800.0 nM 5.42
CHEMBL87976 — IC50 = 3900.0 nM 5.41
CHEMBL88100 — IC50 = 4400.0 nM 5.36
CHEMBL85970 — IC50 = 4900.0 nM 5.31
CHEMBL87043 — IC50 = 6000.0 nM 5.22
CHEMBL86678 — IC50 = 6400.0 nM 5.19
CHEMBL315851 — IC50 = 7700.0 nM 5.11
CHEMBL314362 — IC50 = 10000.0 nM 5.00