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Assay Detail

CHEMBL829510

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

Binding
Inhibitory concentration against recombinant human caspase-7 in neuronal precursor (NT2) cells
ChEMBL ↗
50
Total Activities
50
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-7 (CHEMBL3468) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors.
Han Y, Giroux A, Colucci J, Bayly CI, Mckay DJ, Roy S, Xanthoudakis S, Vaillancourt J, Rasper DM, Tam J, Tawa P, Nicholson DW, Zamboni RJ.
Bioorg Med Chem Lett (2005) 15 : 1173 -1180
PubMed 15686936 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 6.43 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL443565 — — 1 8.10
CHEMBL178116 — — 1 8.00
CHEMBL366927 — — 1 7.89
CHEMBL180669 — — 1 7.44
CHEMBL361825 — — 1 7.38
CHEMBL180646 — — 1 7.19
CHEMBL360788 — — 1 7.08
CHEMBL362074 — — 1 7.06
CHEMBL179503 — — 1 7.05
CHEMBL178514 — — 1 7.00
CHEMBL181623 — — 1 6.96
CHEMBL425699 — — 1 6.92
CHEMBL179551 — — 1 6.89
CHEMBL367356 — — 1 6.89
CHEMBL434147 — — 1 6.89
CHEMBL359598 — — 1 6.85
CHEMBL180623 — — 1 6.85
CHEMBL178674 — — 1 6.58
CHEMBL181027 — — 1 6.51
CHEMBL181763 — — 1 6.50
CHEMBL424789 — — 1 6.39
CHEMBL178339 — — 1 6.32
CHEMBL180273 — — 1 6.31
CHEMBL264344 — — 1 6.27
CHEMBL178775 — — 1 6.27
CHEMBL369290 — — 1 6.22
CHEMBL433771 — — 1 6.14
CHEMBL179066 — — 1 6.12
CHEMBL361613 — — 1 6.09
CHEMBL441118 — — 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL443565 — IC50 = 8.0 nM 8.10
CHEMBL178116 — IC50 = 10.0 nM 8.00
CHEMBL366927 — IC50 = 13.0 nM 7.89
CHEMBL180669 — IC50 = 36.0 nM 7.44
CHEMBL361825 — IC50 = 42.0 nM 7.38
CHEMBL180646 — IC50 = 65.0 nM 7.19
CHEMBL360788 — IC50 = 83.0 nM 7.08
CHEMBL362074 — IC50 = 87.0 nM 7.06
CHEMBL179503 — IC50 = 90.0 nM 7.05
CHEMBL178514 — IC50 = 100.0 nM 7.00
CHEMBL181623 — IC50 = 110.0 nM 6.96
CHEMBL425699 — IC50 = 120.0 nM 6.92
CHEMBL434147 — IC50 = 130.0 nM 6.89
CHEMBL367356 — IC50 = 130.0 nM 6.89
CHEMBL179551 — IC50 = 130.0 nM 6.89
CHEMBL359598 — IC50 = 140.0 nM 6.85
CHEMBL180623 — IC50 = 140.0 nM 6.85
CHEMBL178674 — IC50 = 260.0 nM 6.58
CHEMBL181027 — IC50 = 310.0 nM 6.51
CHEMBL181763 — IC50 = 320.0 nM 6.50
CHEMBL424789 — IC50 = 410.0 nM 6.39
CHEMBL178339 — IC50 = 480.0 nM 6.32
CHEMBL180273 — IC50 = 490.0 nM 6.31
CHEMBL264344 — IC50 = 540.0 nM 6.27
CHEMBL178775 — IC50 = 540.0 nM 6.27
CHEMBL369290 — IC50 = 600.0 nM 6.22
CHEMBL433771 — IC50 = 730.0 nM 6.14
CHEMBL179066 — IC50 = 750.0 nM 6.12
CHEMBL361613 — IC50 = 810.0 nM 6.09
CHEMBL441118 — IC50 = 840.0 nM 6.08
CHEMBL181295 — IC50 = 1010.0 nM 6.00
CHEMBL360355 — IC50 = 1000.0 nM 6.00
CHEMBL181274 — IC50 = 1040.0 nM 5.98
CHEMBL181768 — IC50 = 1130.0 nM 5.95
CHEMBL181775 — IC50 = 2420.0 nM 5.62
CHEMBL180763 — IC50 = 2540.0 nM 5.59
CHEMBL361983 — IC50 = 2600.0 nM 5.58
CHEMBL181396 — IC50 = 3240.0 nM 5.49
CHEMBL362213 — IC50 = 3280.0 nM 5.48
CHEMBL360956 — IC50 = 4680.0 nM 5.33
CHEMBL362191 — IC50 = 5170.0 nM 5.29
CHEMBL359643 — IC50 = 9730.0 nM 5.01
CHEMBL181948 — IC50 = 9710.0 nM 5.01
CHEMBL178280 — IC50 > 10000.0 nM -
CHEMBL220238 — IC50 > 10000.0 nM -
CHEMBL182103 — IC50 > 10000.0 nM -
CHEMBL359542 — IC50 > 10000.0 nM -
CHEMBL447233 — IC50 > 10000.0 nM -
CHEMBL360020 — IC50 > 10000.0 nM -
CHEMBL360915 — IC50 > 10000.0 nM -