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Assay Detail

CHEMBL820592

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

Binding
Inhibitory activity against Tumor necrosis factor alpha-converting enzyme (TACE) in blood.
ChEMBL ↗
71
Total Activities
71
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Blood
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Disintegrin and metalloproteinase domain-containing protein 17 (CHEMBL3706) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors.
Barlaam B, Bird TG, Lambert-Van Der Brempt C, Campbell D, Foster SJ, Maciewicz R.
J Med Chem (1999) 42 : 4890 -4908
PubMed 10579851 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 71 8.71 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL432079 — — 1 9.70
CHEMBL147956 — — 1 9.68
CHEMBL439983 — — 1 9.64
CHEMBL357203 — — 1 9.48
CHEMBL148373 — — 1 9.48
CHEMBL144188 — — 1 9.40
CHEMBL144736 — — 1 9.38
CHEMBL144229 — — 1 9.37
CHEMBL144101 — — 1 9.36
CHEMBL144363 — — 1 9.27
CHEMBL144001 — — 1 9.24
CHEMBL342100 — — 1 9.24
CHEMBL344312 — — 1 9.22
CHEMBL344060 — — 1 9.21
CHEMBL342069 — — 1 9.20
CHEMBL144283 — — 1 9.18
CHEMBL147383 — — 1 9.10
CHEMBL147051 — — 1 9.10
CHEMBL148331 — — 1 9.10
CHEMBL29976 — — 1 9.00
CHEMBL144611 — — 1 9.00
CHEMBL359217 — — 1 9.00
CHEMBL145128 — — 1 9.00
CHEMBL435683 — — 1 9.00
CHEMBL148395 — — 1 8.96
CHEMBL436609 — — 1 8.96
CHEMBL145069 — — 1 8.92
CHEMBL147797 — — 1 8.92
CHEMBL357898 — — 1 8.90
CHEMBL357446 — — 1 8.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL432079 — IC50 = 0.2 nM 9.70
CHEMBL147956 — IC50 = 0.21 nM 9.68
CHEMBL439983 — IC50 = 0.23 nM 9.64
CHEMBL357203 — IC50 = 0.33 nM 9.48
CHEMBL148373 — IC50 = 0.33 nM 9.48
CHEMBL144188 — IC50 = 0.4 nM 9.40
CHEMBL144736 — IC50 = 0.42 nM 9.38
CHEMBL144229 — IC50 = 0.43 nM 9.37
CHEMBL144101 — IC50 = 0.44 nM 9.36
CHEMBL144363 — IC50 = 0.54 nM 9.27
CHEMBL144001 — IC50 = 0.57 nM 9.24
CHEMBL342100 — IC50 = 0.57 nM 9.24
CHEMBL344312 — IC50 = 0.6 nM 9.22
CHEMBL344060 — IC50 = 0.61 nM 9.21
CHEMBL342069 — IC50 = 0.63 nM 9.20
CHEMBL144283 — IC50 = 0.66 nM 9.18
CHEMBL147383 — IC50 = 0.79 nM 9.10
CHEMBL147051 — IC50 = 0.8 nM 9.10
CHEMBL148331 — IC50 = 0.8 nM 9.10
CHEMBL29976 — IC50 = 1.0 nM 9.00
CHEMBL144611 — IC50 = 1.0 nM 9.00
CHEMBL359217 — IC50 = 1.0 nM 9.00
CHEMBL145128 — IC50 = 1.0 nM 9.00
CHEMBL435683 — IC50 = 1.0 nM 9.00
CHEMBL436609 — IC50 = 1.1 nM 8.96
CHEMBL148395 — IC50 = 1.1 nM 8.96
CHEMBL145069 — IC50 = 1.2 nM 8.92
CHEMBL147797 — IC50 = 1.2 nM 8.92
CHEMBL357898 — IC50 = 1.25 nM 8.90
CHEMBL357446 — IC50 = 1.3 nM 8.89
CHEMBL144780 — IC50 = 1.3 nM 8.89
CHEMBL357414 — IC50 = 1.3 nM 8.89
CHEMBL358129 — IC50 = 1.4 nM 8.85
CHEMBL147149 — IC50 = 1.4 nM 8.85
CHEMBL145836 — IC50 = 1.5 nM 8.82
CHEMBL356259 — IC50 = 1.5 nM 8.82
CHEMBL424492 — IC50 = 1.5 nM 8.82
CHEMBL357195 — IC50 = 1.5 nM 8.82
CHEMBL355900 — IC50 = 1.6 nM 8.80
CHEMBL147091 — IC50 = 1.6 nM 8.80
CHEMBL344759 — IC50 = 1.6 nM 8.80
CHEMBL114427 — IC50 = 1.8 nM 8.74
CHEMBL144568 — IC50 = 2.0 nM 8.70
CHEMBL146326 — IC50 = 2.1 nM 8.68
CHEMBL147542 — IC50 = 2.2 nM 8.66
CHEMBL144206 — IC50 = 2.8 nM 8.55
CHEMBL144021 — IC50 = 2.8 nM 8.55
CHEMBL144857 — IC50 = 2.8 nM 8.55
CHEMBL343021 — IC50 = 2.9 nM 8.54
CHEMBL144293 — IC50 = 3.1 nM 8.51