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Assay Detail

CHEMBL1049047

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

Functional
Inhibition of antigen-stimulated IL-2 production in human Jurkat cells expressing MART-1 antigen specific TCR
31
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Jurkat (CHEMBL397)
Type CELL-LINE
Organism Homo sapiens

Publication

Disubstituted pyrimidines as Lck inhibitors.
Hunt JA, Beresis RT, Goulet JL, Holmes MA, Hong XJ, Kovacs E, Mills SG, Ruzek RD, Wong F, Hermes JD, Park YW, Salowe SP, Sonatore LM, Wu L, Woods A, Zaller DM, Sinclair PJ.
Bioorg Med Chem Lett (2009) 19 : 5440 -5443
PubMed 19674899 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 6.91 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL572197 1 8.10
CHEMBL566284 1 7.80
CHEMBL569240 1 7.71
CHEMBL568759 1 7.38
CHEMBL567881 1 7.24
CHEMBL585573 1 7.07
CHEMBL584721 1 7.01
CHEMBL567029 1 6.96
CHEMBL566813 1 6.96
CHEMBL565933 1 6.96
CHEMBL566582 1 6.89
CHEMBL569496 1 6.81
CHEMBL566373 1 6.78
CHEMBL569052 2 6.44
CHEMBL568762 1 6.27
CHEMBL565263 1 6.26
CHEMBL566507 1 6.07
CHEMBL568326 1 5.68
CHEMBL585574 1 -
CHEMBL568763 1 -
CHEMBL567592 1 -
CHEMBL577469 1 -
CHEMBL569250 1 -
CHEMBL568543 1 -
CHEMBL568542 1 -
CHEMBL568101 1 -
CHEMBL572095 1 -
CHEMBL572079 1 -
CHEMBL572200 1 -
CHEMBL572199 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL572197 IC50 = 8.0 nM 8.10
CHEMBL566284 IC50 = 16.0 nM 7.80
CHEMBL569240 IC50 = 19.5 nM 7.71
CHEMBL568759 IC50 = 42.0 nM 7.38
CHEMBL567881 IC50 = 58.0 nM 7.24
CHEMBL585573 IC50 = 86.0 nM 7.07
CHEMBL584721 IC50 = 98.0 nM 7.01
CHEMBL567029 IC50 = 111.0 nM 6.96
CHEMBL565933 IC50 = 111.0 nM 6.96
CHEMBL566813 IC50 = 111.0 nM 6.96
CHEMBL566582 IC50 = 128.0 nM 6.89
CHEMBL569496 IC50 = 154.0 nM 6.81
CHEMBL566373 IC50 = 167.0 nM 6.78
CHEMBL569052 IC50 = 361.0 nM 6.44
CHEMBL568762 IC50 = 538.0 nM 6.27
CHEMBL565263 IC50 = 546.0 nM 6.26
CHEMBL566507 IC50 = 847.0 nM 6.07
CHEMBL568326 IC50 = 2073.0 nM 5.68
CHEMBL568763 IC50 > 10000.0 nM -
CHEMBL585574 IC50 > 20000.0 nM -
CHEMBL567592 IC50 > 1000.0 nM -
CHEMBL577469 IC50 > 10000.0 nM -
CHEMBL569250 IC50 > 10000.0 nM -
CHEMBL568543 IC50 > 10000.0 nM -
CHEMBL568542 IC50 > 1000.0 nM -
CHEMBL568101 IC50 > 1000.0 nM -
CHEMBL572095 IC50 > 10000.0 nM -
CHEMBL572079 IC50 > 10000.0 nM -
CHEMBL572200 IC50 > 1000.0 nM -
CHEMBL572199 IC50 > 1000.0 nM -
CHEMBL569052 IC50 > 1000.0 nM -