Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4010789

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

Binding
Inhibition of recombinant TACE catalytic domain (unknown origin) using Abz-LAQAVRSSSR-Dpa as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by FRET assay
ChEMBL ↗
96
Total Activities
47
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 96 8.78 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4071465 — — 2 9.40
CHEMBL4094122 — — 2 9.30
CHEMBL4071782 — — 2 9.30
CHEMBL4080774 — — 2 9.22
CHEMBL4097420 — — 2 9.22
CHEMBL4076782 — — 2 9.22
CHEMBL4078142 — — 2 9.22
CHEMBL4069898 — — 2 9.22
CHEMBL4076142 — — 2 9.22
CHEMBL4105513 — — 2 9.22
CHEMBL4105045 — — 2 9.22
CHEMBL4096933 — — 2 9.22
CHEMBL4105634 — — 2 9.22
CHEMBL4100854 — — 2 9.22
CHEMBL4102282 — — 2 9.22
CHEMBL4082009 — — 2 9.22
CHEMBL4084316 — — 2 9.20
CHEMBL4101060 — — 2 9.20
CHEMBL4067381 — — 2 9.10
CHEMBL4099382 — — 2 9.10
CHEMBL4075636 — — 2 9.05
CHEMBL4070236 — — 2 9.00
CHEMBL4077184 — — 2 9.00
CHEMBL4086030 — — 2 9.00
CHEMBL4101507 — — 2 9.00
CHEMBL4069740 — — 2 9.00
CHEMBL4076844 — — 2 8.90
CHEMBL4077594 — — 2 8.90
CHEMBL4089231 — — 2 8.90
CHEMBL4070455 — — 2 8.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4071465 — IC50 = 0.3981 nM 9.40
CHEMBL4071465 — IC50 = 0.4 nM 9.40
CHEMBL4071782 — IC50 = 0.5012 nM 9.30
CHEMBL4071782 — IC50 = 0.5 nM 9.30
CHEMBL4094122 — IC50 = 0.5 nM 9.30
CHEMBL4094122 — IC50 = 0.5012 nM 9.30
CHEMBL4096933 — IC50 = 0.6 nM 9.22
CHEMBL4082009 — IC50 = 0.6 nM 9.22
CHEMBL4105513 — IC50 = 0.6 nM 9.22
CHEMBL4078142 — IC50 = 0.6 nM 9.22
CHEMBL4097420 — IC50 = 0.6 nM 9.22
CHEMBL4102282 — IC50 = 0.6 nM 9.22
CHEMBL4100854 — IC50 = 0.6 nM 9.22
CHEMBL4080774 — IC50 = 0.6 nM 9.22
CHEMBL4076782 — IC50 = 0.6 nM 9.22
CHEMBL4069898 — IC50 = 0.6 nM 9.22
CHEMBL4076142 — IC50 = 0.6 nM 9.22
CHEMBL4105045 — IC50 = 0.6 nM 9.22
CHEMBL4105634 — IC50 = 0.6 nM 9.22
CHEMBL4105513 — IC50 = 0.631 nM 9.20
CHEMBL4082009 — IC50 = 0.631 nM 9.20
CHEMBL4078142 — IC50 = 0.631 nM 9.20
CHEMBL4069898 — IC50 = 0.631 nM 9.20
CHEMBL4097420 — IC50 = 0.631 nM 9.20
CHEMBL4100854 — IC50 = 0.631 nM 9.20
CHEMBL4076142 — IC50 = 0.631 nM 9.20
CHEMBL4080774 — IC50 = 0.631 nM 9.20
CHEMBL4084316 — IC50 = 0.631 nM 9.20
CHEMBL4105045 — IC50 = 0.631 nM 9.20
CHEMBL4102282 — IC50 = 0.631 nM 9.20
CHEMBL4096933 — IC50 = 0.631 nM 9.20
CHEMBL4105634 — IC50 = 0.631 nM 9.20
CHEMBL4076782 — IC50 = 0.631 nM 9.20
CHEMBL4101060 — IC50 = 0.631 nM 9.20
CHEMBL4101060 — IC50 = 0.7 nM 9.15
CHEMBL4084316 — IC50 = 0.7 nM 9.15
CHEMBL4067381 — IC50 = 0.8 nM 9.10
CHEMBL4099382 — IC50 = 0.8 nM 9.10
CHEMBL4099382 — IC50 = 0.7943 nM 9.10
CHEMBL4067381 — IC50 = 0.7943 nM 9.10
CHEMBL4075636 — IC50 = 0.9 nM 9.05
CHEMBL4101507 — IC50 = 1.0 nM 9.00
CHEMBL4077184 — IC50 = 1.0 nM 9.00
CHEMBL4069740 — IC50 = 1.0 nM 9.00
CHEMBL4075636 — IC50 = 1.0 nM 9.00
CHEMBL4077184 — IC50 = 1.0 nM 9.00
CHEMBL4101507 — IC50 = 1.0 nM 9.00
CHEMBL4070236 — IC50 = 1.0 nM 9.00
CHEMBL4086030 — IC50 = 1.0 nM 9.00
CHEMBL4070236 — IC50 = 1.1 nM 8.96