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Assay Detail

CHEMBL828519

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

Binding
Inhibitory activity against recombinant human Caspase-1
30
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Caspase-1 (CHEMBL4801)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Lipophilic versus hydrogen-bonding effect in P3 on potency and selectivity of valine aspartyl ketones as caspase 3 inhibitors.
Mellon C, Aspiotis R, Black CW, Bayly CI, Grimm EL, Giroux A, Han Y, Isabel E, McKay DJ, Nicholson DW, Rasper DM, Roy S, Tam J, Thornberry NA, Vaillancourt JP, Xanthoudakis S, Zamboni R.
Bioorg Med Chem Lett (2005) 15 : 3886 -3890
PubMed 16023344 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 5.34 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183619 1 6.17
CHEMBL183109 2 5.99
CHEMBL183379 1 5.81
CHEMBL361111 1 5.61
CHEMBL182095 1 5.52
CHEMBL82932 2 5.52
CHEMBL2096776 1 5.39
CHEMBL183760 1 5.38
CHEMBL360690 1 5.35
CHEMBL360046 1 5.31
CHEMBL360880 1 5.26
CHEMBL182078 1 5.24
CHEMBL167071 1 5.21
CHEMBL361397 1 5.19
CHEMBL166513 1 5.15
CHEMBL359479 1 5.02
CHEMBL180131 1 4.74
CHEMBL183564 1 4.72
CHEMBL354345 1 4.67
CHEMBL183120 1 -
CHEMBL182295 1 -
CHEMBL360292 1 -
CHEMBL182096 1 -
CHEMBL362695 1 -
CHEMBL367365 1 -
CHEMBL182563 1 -
CHEMBL183655 1 -
CHEMBL181355 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183619 IC50 = 675.0 nM 6.17
CHEMBL183109 IC50 = 1030.0 nM 5.99
CHEMBL183379 IC50 = 1540.0 nM 5.81
CHEMBL361111 IC50 = 2460.0 nM 5.61
CHEMBL182095 IC50 = 3015.0 nM 5.52
CHEMBL82932 IC50 = 3050.0 nM 5.52
CHEMBL82932 IC50 = 3040.0 nM 5.52
CHEMBL2096776 IC50 = 4060.0 nM 5.39
CHEMBL183760 IC50 = 4160.0 nM 5.38
CHEMBL360690 IC50 = 4490.0 nM 5.35
CHEMBL360046 IC50 = 4850.0 nM 5.31
CHEMBL360880 IC50 = 5450.0 nM 5.26
CHEMBL182078 IC50 = 5810.0 nM 5.24
CHEMBL167071 IC50 = 6190.0 nM 5.21
CHEMBL361397 IC50 = 6505.0 nM 5.19
CHEMBL166513 IC50 = 7070.0 nM 5.15
CHEMBL359479 IC50 = 9590.0 nM 5.02
CHEMBL180131 IC50 = 18400.0 nM 4.74
CHEMBL183564 IC50 = 18900.0 nM 4.72
CHEMBL354345 IC50 = 21200.0 nM 4.67
CHEMBL183120 IC50 > 10000.0 nM -
CHEMBL183109 IC50 > 10000.0 nM -
CHEMBL360292 IC50 > 10000.0 nM -
CHEMBL182096 IC50 > 10000.0 nM -
CHEMBL362695 IC50 > 10000.0 nM -
CHEMBL367365 IC50 > 10000.0 nM -
CHEMBL182563 IC50 > 10000.0 nM -
CHEMBL183655 IC50 > 10000.0 nM -
CHEMBL181355 IC50 > 10000.0 nM -
CHEMBL182295 IC50 > 10000.0 nM -