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Assay Detail

CHEMBL1764809

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Binding
Inhibition of caspase 6 by fluorometric assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Caspase-6 (CHEMBL3308)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of isatin analogs as caspase-3 inhibitors: introduction of a hydrophilic group increases potency in a whole cell assay.
Chu W, Rothfuss J, Zhou D, Mach RH.
Bioorg Med Chem Lett (2011) 21 : 2192 -2197
PubMed 21441025 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.61 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL478081 1 8.10
CHEMBL1762357 1 6.35
CHEMBL1762356 1 6.29
CHEMBL1762354 1 6.13
CHEMBL1762360 1 6.11
CHEMBL1762358 1 6.03
CHEMBL1762355 1 6.00
CHEMBL1762359 1 5.93
CHEMBL1762348 1 5.53
CHEMBL1762364 1 5.46
CHEMBL456799 1 5.35
CHEMBL1762366 1 5.33
CHEMBL1762346 1 5.31
CHEMBL1762353 1 5.16
CHEMBL1762361 1 5.16
CHEMBL1762352 1 5.12
CHEMBL1762362 1 5.11
CHEMBL1762349 1 5.06
CHEMBL1762350 1 5.04
CHEMBL1762365 1 5.04
CHEMBL456798 1 5.00
CHEMBL1762363 1 4.87
CHEMBL1762351 1 -
CHEMBL1762347 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL478081 IC50 = 8.0 nM 8.10
CHEMBL1762357 IC50 = 450.0 nM 6.35
CHEMBL1762356 IC50 = 509.0 nM 6.29
CHEMBL1762354 IC50 = 747.0 nM 6.13
CHEMBL1762360 IC50 = 770.0 nM 6.11
CHEMBL1762358 IC50 = 927.0 nM 6.03
CHEMBL1762355 IC50 = 1012.0 nM 6.00
CHEMBL1762359 IC50 = 1165.0 nM 5.93
CHEMBL1762348 IC50 = 2987.0 nM 5.53
CHEMBL1762364 IC50 = 3475.0 nM 5.46
CHEMBL456799 IC50 = 4425.0 nM 5.35
CHEMBL1762366 IC50 = 4700.0 nM 5.33
CHEMBL1762346 IC50 = 4930.0 nM 5.31
CHEMBL1762353 IC50 = 6900.0 nM 5.16
CHEMBL1762361 IC50 = 6950.0 nM 5.16
CHEMBL1762352 IC50 = 7666.0 nM 5.12
CHEMBL1762362 IC50 = 7750.0 nM 5.11
CHEMBL1762349 IC50 = 8700.0 nM 5.06
CHEMBL1762350 IC50 = 9200.0 nM 5.04
CHEMBL1762365 IC50 = 9125.0 nM 5.04
CHEMBL456798 IC50 = 9967.0 nM 5.00
CHEMBL1762363 IC50 = 13450.0 nM 4.87
CHEMBL1762351 IC50 > 10000.0 nM -
CHEMBL1762347 IC50 > 10000.0 nM -