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Assay Detail

CHEMBL3880445

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

Binding
Inhibition of aggrecanase in primary porcine chondrocytes assessed as inhibition of 35S-proteoglycan release measured after 9 to 12 hrs by liquid scintillation counting method
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Aggrecanase (CHEMBL3988627)
Type PROTEIN FAMILY
Organism Sus scrofa

Publication

Selective inhibitors of aggrecanase in osteoarthritis treatment
(2001)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.93 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3905996 1 8.00
CHEMBL3910163 1 8.00
CHEMBL186500 1 8.00
CHEMBL3909799 1 8.00
CHEMBL3899940 1 8.00
CHEMBL363126 1 8.00
CHEMBL3968787 1 8.00
CHEMBL182306 1 8.00
CHEMBL372261 1 8.00
CHEMBL3985409 1 7.27
CHEMBL179552 1 -
CHEMBL3954431 1 -
CHEMBL3897970 1 -
CHEMBL3895305 1 -
CHEMBL372878 1 -
CHEMBL365283 1 -
CHEMBL3981624 1 -
CHEMBL3979213 1 -
CHEMBL3921667 1 -
CHEMBL187092 1 -
CHEMBL186663 1 -
CHEMBL190415 1 -
CHEMBL3902100 1 -
CHEMBL3955144 1 -
CHEMBL183474 1 -
CHEMBL189216 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3905996 IC50 = 10.0 nM 8.00
CHEMBL3910163 IC50 = 10.0 nM 8.00
CHEMBL186500 IC50 = 10.0 nM 8.00
CHEMBL3909799 IC50 = 10.0 nM 8.00
CHEMBL3899940 IC50 = 10.0 nM 8.00
CHEMBL363126 IC50 = 10.0 nM 8.00
CHEMBL3968787 IC50 = 10.0 nM 8.00
CHEMBL182306 IC50 = 10.0 nM 8.00
CHEMBL372261 IC50 = 10.0 nM 8.00
CHEMBL3985409 IC50 = 53.5 nM 7.27
CHEMBL179552 IC50 < 10.0 nM -
CHEMBL3954431 IC50 < 10.0 nM -
CHEMBL3897970 IC50 < 10.0 nM -
CHEMBL3895305 IC50 < 10.0 nM -
CHEMBL372878 IC50 < 10.0 nM -
CHEMBL365283 IC50 < 10.0 nM -
CHEMBL3981624 IC50 < 10.0 nM -
CHEMBL3979213 IC50 < 10.0 nM -
CHEMBL3921667 IC50 < 10.0 nM -
CHEMBL187092 IC50 < 10.0 nM -
CHEMBL186663 IC50 < 10.0 nM -
CHEMBL190415 IC50 < 10.0 nM -
CHEMBL3902100 IC50 < 10.0 nM -
CHEMBL3955144 IC50 < 10.0 nM -
CHEMBL183474 IC50 < 10.0 nM -
CHEMBL189216 IC50 < 10.0 nM -