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Assay Detail

CHEMBL705832

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Functional
Inhibition of AP-1 (activator protein-1) mediated transcriptional activation in Jurkat T-cells
ChEMBL ↗
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Jurkat
Confidence 7 — Homologous single protein target
Curated By Expert

Target

Transcription factor AP1 (CHEMBL2111421) ↗
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Novel inhibitors of AP-1 and NF-kappaB mediated gene expression: structure-activity relationship studies of ethyl 4-[(3-methyl-2,5-dioxo(3-pyrrolinyl))amino]-2-(trifluoromethyl)++ +pyrimidi ne-5-carboxylate.
Palanki MS, Erdman PE, Manning AM, Ow A, Ransone LJ, Spooner C, Suto C, Suto M.
Bioorg Med Chem Lett (2000) 10 : 1645 -1648
PubMed 10937715 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 5.84 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL43549 — — 1 7.70
CHEMBL43610 — — 1 7.00
CHEMBL42952 — — 1 7.00
CHEMBL43534 — — 1 6.70
CHEMBL42650 — — 1 6.70
CHEMBL295508 — — 1 6.70
CHEMBL295192 — — 1 6.70
CHEMBL44525 — — 1 6.70
CHEMBL42204 — — 1 6.52
CHEMBL296695 — — 1 6.52
CHEMBL43259 — — 1 6.52
CHEMBL296202 — — 1 6.52
CHEMBL45261 — — 1 6.52
CHEMBL295050 — — 1 6.40
CHEMBL43451 — — 1 6.16
CHEMBL43251 — — 1 6.16
CHEMBL42079 — — 1 6.16
CHEMBL297842 — — 1 6.05
CHEMBL46509 — — 1 6.00
CHEMBL413028 — — 1 6.00
CHEMBL42719 — — 1 6.00
CHEMBL42235 — — 1 6.00
CHEMBL42547 — — 1 6.00
CHEMBL43388 — — 1 5.70
CHEMBL44089 — — 1 5.70
CHEMBL416627 — — 1 5.70
CHEMBL43550 — — 1 5.52
CHEMBL297420 — — 1 5.40
CHEMBL43199 — — 1 5.40
CHEMBL42503 — — 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL43549 — IC50 = 20.0 nM 7.70
CHEMBL43610 — IC50 = 100.0 nM 7.00
CHEMBL42952 — IC50 = 100.0 nM 7.00
CHEMBL43534 — IC50 = 200.0 nM 6.70
CHEMBL42650 — IC50 = 200.0 nM 6.70
CHEMBL295508 — IC50 = 200.0 nM 6.70
CHEMBL295192 — IC50 = 200.0 nM 6.70
CHEMBL44525 — IC50 = 200.0 nM 6.70
CHEMBL43259 — IC50 = 300.0 nM 6.52
CHEMBL45261 — IC50 = 300.0 nM 6.52
CHEMBL296202 — IC50 = 300.0 nM 6.52
CHEMBL296695 — IC50 = 300.0 nM 6.52
CHEMBL42204 — IC50 = 300.0 nM 6.52
CHEMBL295050 — IC50 = 400.0 nM 6.40
CHEMBL42079 — IC50 = 700.0 nM 6.16
CHEMBL43451 — IC50 = 700.0 nM 6.16
CHEMBL43251 — IC50 = 700.0 nM 6.16
CHEMBL297842 — IC50 = 900.0 nM 6.05
CHEMBL42547 — IC50 = 1000.0 nM 6.00
CHEMBL42235 — IC50 = 1000.0 nM 6.00
CHEMBL413028 — IC50 = 1000.0 nM 6.00
CHEMBL46509 — IC50 = 1000.0 nM 6.00
CHEMBL42719 — IC50 = 1000.0 nM 6.00
CHEMBL43388 — IC50 = 2000.0 nM 5.70
CHEMBL44089 — IC50 = 2000.0 nM 5.70
CHEMBL416627 — IC50 = 2000.0 nM 5.70
CHEMBL43550 — IC50 = 3000.0 nM 5.52
CHEMBL297420 — IC50 = 4000.0 nM 5.40
CHEMBL43199 — IC50 = 4000.0 nM 5.40
CHEMBL42503 — IC50 = 5000.0 nM 5.30
CHEMBL290202 — IC50 = 5000.0 nM 5.30
CHEMBL42815 — IC50 = 6000.0 nM 5.22
CHEMBL298245 — IC50 = 6000.0 nM 5.22
CHEMBL298418 — IC50 = 7000.0 nM 5.16
CHEMBL296896 — IC50 = 7000.0 nM 5.16
CHEMBL43158 — IC50 = 8000.0 nM 5.10
CHEMBL42687 — IC50 = 10000.0 nM 5.00
CHEMBL42000 — IC50 = 10000.0 nM 5.00
CHEMBL43606 — IC50 = 10000.0 nM 5.00
CHEMBL47053 — IC50 = 10000.0 nM 5.00
CHEMBL43619 — IC50 = 10000.0 nM 5.00
CHEMBL290176 — IC50 = 10000.0 nM 5.00
CHEMBL42167 — IC50 = 15000.0 nM 4.82
CHEMBL431718 — IC50 = 16000.0 nM 4.80
CHEMBL290656 — IC50 = 20000.0 nM 4.70