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Assay Detail

CHEMBL896780

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

Binding
Inhibition of human S1P expressed in CHOK1 cells
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Membrane-bound transcription factor site-1 protease (CHEMBL5916)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Aminopyrrolidineamide inhibitors of site-1 protease.
Hay BA, Abrams B, Zumbrunn AY, Valentine JJ, Warren LC, Petras SF, Shelly LD, Xia A, Varghese AH, Hawkins JL, Van Camp JA, Robbins MD, Landschulz K, Harwood HJ.
Bioorg Med Chem Lett (2007) 17 : 4411 -4414
PubMed 17583500 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 6.43 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL391935 1 8.10
CHEMBL233987 1 7.54
CHEMBL233799 1 7.43
CHEMBL233421 1 7.02
CHEMBL233422 1 7.00
CHEMBL233609 1 6.85
CHEMBL233610 1 6.80
CHEMBL233611 1 6.77
CHEMBL394028 1 6.60
CHEMBL393989 1 6.51
CHEMBL232587 1 6.37
CHEMBL232777 1 6.29
CHEMBL231776 1 6.27
CHEMBL233573 1 6.23
CHEMBL233572 1 6.08
CHEMBL394029 1 6.01
CHEMBL232577 1 5.85
CHEMBL393377 1 5.80
CHEMBL232776 1 5.43
CHEMBL233165 1 5.05
CHEMBL233166 1 5.02
CHEMBL232778 1 -
CHEMBL397866 1 -
CHEMBL233574 1 -
CHEMBL233419 1 -
CHEMBL233605 1 -
CHEMBL233606 1 -
CHEMBL233607 1 -
CHEMBL233797 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL391935 IC50 = 8.0 nM 8.10
CHEMBL233987 IC50 = 29.0 nM 7.54
CHEMBL233799 IC50 = 37.0 nM 7.43
CHEMBL233421 IC50 = 95.0 nM 7.02
CHEMBL233422 IC50 = 100.0 nM 7.00
CHEMBL233609 IC50 = 140.0 nM 6.85
CHEMBL233610 IC50 = 160.0 nM 6.80
CHEMBL233611 IC50 = 170.0 nM 6.77
CHEMBL394028 IC50 = 250.0 nM 6.60
CHEMBL393989 IC50 = 310.0 nM 6.51
CHEMBL232587 IC50 = 430.0 nM 6.37
CHEMBL232777 IC50 = 510.0 nM 6.29
CHEMBL231776 IC50 = 540.0 nM 6.27
CHEMBL233573 IC50 = 590.0 nM 6.23
CHEMBL233572 IC50 = 840.0 nM 6.08
CHEMBL394029 IC50 = 970.0 nM 6.01
CHEMBL232577 IC50 = 1400.0 nM 5.85
CHEMBL393377 IC50 = 1600.0 nM 5.80
CHEMBL232776 IC50 = 3700.0 nM 5.43
CHEMBL233165 IC50 = 9000.0 nM 5.05
CHEMBL233166 IC50 = 9600.0 nM 5.02
CHEMBL232778 IC50 > 16000.0 nM -
CHEMBL397866 IC50 > 30000.0 nM -
CHEMBL233574 IC50 > 5000.0 nM -
CHEMBL233419 IC50 > 30000.0 nM -
CHEMBL233605 IC50 > 30000.0 nM -
CHEMBL233606 IC50 > 30000.0 nM -
CHEMBL233607 IC50 > 30000.0 nM -
CHEMBL233797 IC50 > 30000.0 nM -