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Assay Detail

CHEMBL5328252

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Binding
Binding affinity to FLAG-tagged human TIMP3 expressed in HEK293 cells assessed as dissociation constant
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Metalloproteinase inhibitor 3 (CHEMBL5465289)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Suramin analogues protect cartilage against osteoarthritic breakdown by increasing levels of tissue inhibitor of metalloproteinases 3 (TIMP-3) in the tissue.
Green J, Tinson RAJ, Betts JHJ, Piras M, Pelut A, Steverding D, Wren SP, Searcey M, Troeberg L.
Bioorg Med Chem (2023) 92 : 117424 -117424
PubMed 37517101 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 8.45 9.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5421682 1 9.07
CHEMBL1207514 1 8.81
CHEMBL265502 SURAMIN 3.0 1 8.72
CHEMBL1615557 1 8.33
CHEMBL4300424 1 8.16
CHEMBL1206126 1 7.58
CHEMBL5420893 1 -
CHEMBL5408018 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5421682 Kd = 0.85 nM 9.07
CHEMBL1207514 Kd = 1.55 nM 8.81
CHEMBL265502 SURAMIN Kd = 1.9 nM 8.72
CHEMBL1615557 Kd = 4.66 nM 8.33
CHEMBL4300424 Kd = 6.88 nM 8.16
CHEMBL1206126 Kd = 26.5 nM 7.58
CHEMBL5420893 Kd > 100.0 nM -
CHEMBL5408018 Kd > 100.0 nM -