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Assay Detail

CHEMBL3829987

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

Binding
Inhibition of ADAM8 (unknown origin) expressed in African green monkey COS7 cells co-expressing CD23 assessed as inhibition of CD23 shedding after 6 hrs by ELISA
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Synthesis and biological evaluation of analogues of the potent ADAM8 inhibitor cyclo(RLsKDK) for the treatment of inflammatory diseases and cancer metastasis.
Yim V, Noisier AF, Hung KY, Bartsch JW, Schlomann U, Brimble MA.
Bioorg Med Chem (2016) 24 : 4032 -4037
PubMed 27407033 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.37 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3828456 1 6.85
CHEMBL3828497 1 6.80
CHEMBL3827732 1 6.72
CHEMBL3827980 1 6.66
CHEMBL3827893 1 6.62
CHEMBL3827446 1 6.59
CHEMBL3827091 1 6.43
CHEMBL3827647 1 6.42
CHEMBL3828432 1 6.38
CHEMBL3827027 1 6.34
CHEMBL3827271 1 6.05
CHEMBL3828603 1 5.91
CHEMBL3827625 1 5.78
CHEMBL3827487 1 5.63
CHEMBL3827100 1 -
CHEMBL3828319 1 -
CHEMBL3827131 1 -
CHEMBL3828248 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3828456 IC50 = 142.0 nM 6.85
CHEMBL3828497 IC50 = 157.0 nM 6.80
CHEMBL3827732 IC50 = 192.0 nM 6.72
CHEMBL3827980 IC50 = 220.0 nM 6.66
CHEMBL3827893 IC50 = 240.0 nM 6.62
CHEMBL3827446 IC50 = 256.0 nM 6.59
CHEMBL3827091 IC50 = 368.0 nM 6.43
CHEMBL3827647 IC50 = 378.0 nM 6.42
CHEMBL3828432 IC50 = 420.0 nM 6.38
CHEMBL3827027 IC50 = 452.0 nM 6.34
CHEMBL3827271 IC50 = 890.0 nM 6.05
CHEMBL3828603 IC50 = 1245.0 nM 5.91
CHEMBL3827625 IC50 = 1645.0 nM 5.78
CHEMBL3827487 IC50 = 2345.0 nM 5.63
CHEMBL3827100 IC50 > 5000.0 nM -
CHEMBL3828319 IC50 > 5000.0 nM -
CHEMBL3827131 IC50 > 5000.0 nM -
CHEMBL3828248 IC50 > 10000.0 nM -