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Assay Detail

CHEMBL640575

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

Binding
In vitro inhibitory activity against human Jurkat T-Cells stably transfected with activating transcription factor 1
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Jurkat
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cyclic AMP-dependent transcription factor ATF-1 (CHEMBL3255)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3',5'- bis(trifluoromethyl)phenyl)-carboxamide: a potent inhibitor of NF-kappa B- and AP-1-mediated gene expression identified using solution-phase combinatorial chemistry.
Sullivan RW, Bigam CG, Erdman PE, Palanki MS, Anderson DW, Goldman ME, Ransone LJ, Suto MJ.
J Med Chem (1998) 41 : 413 -419
PubMed 9484492 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 6.02 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL336546 1 7.30
CHEMBL131636 1 6.92
CHEMBL134490 1 6.82
CHEMBL135133 1 6.31
CHEMBL334485 1 6.30
CHEMBL336099 1 6.30
CHEMBL423153 1 6.18
CHEMBL134603 1 6.05
CHEMBL133940 1 5.92
CHEMBL337482 1 5.92
CHEMBL131789 1 5.80
CHEMBL131622 1 5.57
CHEMBL134990 1 5.55
CHEMBL337695 1 5.52
CHEMBL337516 1 5.52
CHEMBL131976 1 5.52
CHEMBL335697 1 5.42
CHEMBL335655 1 5.40
CHEMBL134522 1 -
CHEMBL335703 1 -
CHEMBL134876 1 -
CHEMBL134773 1 -
CHEMBL335080 1 -
CHEMBL133159 1 -
CHEMBL134776 1 -
CHEMBL132257 1 -
CHEMBL424086 1 -
CHEMBL131741 1 -
CHEMBL134576 1 -
CHEMBL134863 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL336546 IC50 = 50.0 nM 7.30
CHEMBL131636 IC50 = 120.0 nM 6.92
CHEMBL134490 IC50 = 150.0 nM 6.82
CHEMBL135133 IC50 = 490.0 nM 6.31
CHEMBL334485 IC50 = 500.0 nM 6.30
CHEMBL336099 IC50 = 500.0 nM 6.30
CHEMBL423153 IC50 = 660.0 nM 6.18
CHEMBL134603 IC50 = 900.0 nM 6.05
CHEMBL133940 IC50 = 1200.0 nM 5.92
CHEMBL337482 IC50 = 1200.0 nM 5.92
CHEMBL131789 IC50 = 1600.0 nM 5.80
CHEMBL131622 IC50 = 2700.0 nM 5.57
CHEMBL134990 IC50 = 2800.0 nM 5.55
CHEMBL337695 IC50 = 3000.0 nM 5.52
CHEMBL131976 IC50 = 3000.0 nM 5.52
CHEMBL337516 IC50 = 3000.0 nM 5.52
CHEMBL335697 IC50 = 3800.0 nM 5.42
CHEMBL335655 IC50 = 4000.0 nM 5.40
CHEMBL133044 IC50 > 10000.0 nM -
CHEMBL134863 IC50 > 10000.0 nM -
CHEMBL134576 IC50 > 10000.0 nM -
CHEMBL131741 IC50 > 10000.0 nM -
CHEMBL424086 IC50 > 10000.0 nM -
CHEMBL132257 IC50 > 10000.0 nM -
CHEMBL134776 IC50 > 10000.0 nM -
CHEMBL133159 IC50 > 10000.0 nM -
CHEMBL335080 IC50 > 10000.0 nM -
CHEMBL134773 IC50 > 10000.0 nM -
CHEMBL134876 IC50 > 10000.0 nM -
CHEMBL335703 IC50 > 10000.0 nM -
CHEMBL134522 IC50 > 10000.0 nM -