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Assay Detail

CHEMBL4010787

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Binding
Inhibition of TACE (unknown origin)
ChEMBL ↗
32
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification of novel TACE inhibitors compatible with topical application.
Ouvry G, Berton Y, Bhurruth-Alcor Y, Bonnary L, Bouix-Peter C, Bouquet K, Bourotte M, Chambon S, Comino C, Deprez B, Duvert D, Duvert G, Hacini-Rachinel F, Harris CS, Luzy AP, Mathieu A, Millois C, Pascau J, Pinto A, Polge G, Reitz A, Reversé K, Rosignoli C, Taquet N, Hennequin LF.
Bioorg Med Chem Lett (2017) 27 : 1848 -1853
PubMed 28274635 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.89 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95305 — — 2 8.82
CHEMBL98770 — — 2 8.60
CHEMBL318860 — — 2 8.50
CHEMBL318005 — — 2 8.30
CHEMBL99103 — — 2 8.22
CHEMBL99120 — — 2 8.20
CHEMBL421009 — — 2 8.20
CHEMBL95718 — — 2 8.12
CHEMBL318484 — — 2 8.10
CHEMBL99283 — — 2 7.92
CHEMBL329302 — — 2 7.50
CHEMBL99318 — — 2 7.40
CHEMBL329232 — — 2 7.30
CHEMBL316725 — — 2 7.13
CHEMBL98304 — — 2 7.10
CHEMBL99547 — — 2 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95305 — IC50 = 1.5 nM 8.82
CHEMBL95305 — IC50 = 1.585 nM 8.80
CHEMBL98770 — IC50 = 2.512 nM 8.60
CHEMBL98770 — IC50 = 2.7 nM 8.57
CHEMBL318860 — IC50 = 3.162 nM 8.50
CHEMBL318860 — IC50 = 3.4 nM 8.47
CHEMBL318005 — IC50 = 5.012 nM 8.30
CHEMBL318005 — IC50 = 5.2 nM 8.28
CHEMBL99103 — IC50 = 6.0 nM 8.22
CHEMBL421009 — IC50 = 6.31 nM 8.20
CHEMBL99103 — IC50 = 6.31 nM 8.20
CHEMBL99120 — IC50 = 6.31 nM 8.20
CHEMBL421009 — IC50 = 6.5 nM 8.19
CHEMBL99120 — IC50 = 6.8 nM 8.17
CHEMBL95718 — IC50 = 7.6 nM 8.12
CHEMBL318484 — IC50 = 7.9 nM 8.10
CHEMBL318484 — IC50 = 7.943 nM 8.10
CHEMBL95718 — IC50 = 7.943 nM 8.10
CHEMBL99283 — IC50 = 12.0 nM 7.92
CHEMBL99283 — IC50 = 12.59 nM 7.90
CHEMBL329302 — IC50 = 31.62 nM 7.50
CHEMBL329302 — IC50 = 33.0 nM 7.48
CHEMBL99318 — IC50 = 39.81 nM 7.40
CHEMBL99318 — IC50 = 43.0 nM 7.37
CHEMBL329232 — IC50 = 50.12 nM 7.30
CHEMBL329232 — IC50 = 55.0 nM 7.26
CHEMBL316725 — IC50 = 74.0 nM 7.13
CHEMBL316725 — IC50 = 79.43 nM 7.10
CHEMBL98304 — IC50 = 79.43 nM 7.10
CHEMBL98304 — IC50 = 87.0 nM 7.06
CHEMBL99547 — IC50 = 96.0 nM 7.02
CHEMBL99547 — IC50 = 100.0 nM 7.00