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Assay Detail

CHEMBL4010790

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

Binding
Inhibition of TACE in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated TNFalpha production pretreated for 1 hr followed by LPS stimulation for 4 hrs by ELISA
ChEMBL ↗
96
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Disintegrin and metalloproteinase domain-containing protein 17 (CHEMBL4379) ↗
Type SINGLE PROTEIN
Organism Mus musculus

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 6.90 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4067381 — — 2 8.20
CHEMBL4078142 — — 2 8.05
CHEMBL4070236 — — 2 8.00
CHEMBL4105634 — — 2 7.92
CHEMBL4099382 — — 2 7.80
CHEMBL4097420 — — 2 7.75
CHEMBL4074005 — — 4 7.75
CHEMBL4076142 — — 2 7.72
CHEMBL4075636 — — 2 7.70
CHEMBL4077184 — — 2 7.70
CHEMBL4069740 — — 2 7.70
CHEMBL4102282 — — 2 7.70
CHEMBL4105513 — — 2 7.62
CHEMBL4080774 — — 2 7.60
CHEMBL4100854 — — 2 7.52
CHEMBL4096933 — — 2 7.42
CHEMBL4086030 — — 2 7.30
CHEMBL4089231 — — 2 7.30
CHEMBL4070455 — — 2 7.24
CHEMBL4101060 — — 2 7.24
CHEMBL4093788 — — 2 7.22
CHEMBL4071465 — — 2 7.10
CHEMBL4101507 — — 2 7.10
CHEMBL4084316 — — 2 7.05
CHEMBL4061058 — — 2 7.05
CHEMBL4082009 — — 2 7.03
CHEMBL4077726 — — 2 6.80
CHEMBL4076790 — — 2 6.75
CHEMBL4075836 — — 2 6.70
CHEMBL4069898 — — 2 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4067381 — IC50 = 6.31 nM 8.20
CHEMBL4067381 — IC50 = 7.0 nM 8.15
CHEMBL4078142 — IC50 = 9.0 nM 8.05
CHEMBL4070236 — IC50 = 10.0 nM 8.00
CHEMBL4070236 — IC50 = 10.0 nM 8.00
CHEMBL4078142 — IC50 = 10.0 nM 8.00
CHEMBL4105634 — IC50 = 12.0 nM 7.92
CHEMBL4105634 — IC50 = 12.59 nM 7.90
CHEMBL4099382 — IC50 = 15.85 nM 7.80
CHEMBL4099382 — IC50 = 17.0 nM 7.77
CHEMBL4074005 — IC50 = 18.0 nM 7.75
CHEMBL4097420 — IC50 = 18.0 nM 7.75
CHEMBL4076142 — IC50 = 19.0 nM 7.72
CHEMBL4102282 — IC50 = 20.0 nM 7.70
CHEMBL4075636 — IC50 = 20.0 nM 7.70
CHEMBL4102282 — IC50 = 19.95 nM 7.70
CHEMBL4097420 — IC50 = 19.95 nM 7.70
CHEMBL4076142 — IC50 = 19.95 nM 7.70
CHEMBL4074005 — IC50 = 19.95 nM 7.70
CHEMBL4077184 — IC50 = 19.95 nM 7.70
CHEMBL4075636 — IC50 = 19.95 nM 7.70
CHEMBL4069740 — IC50 = 19.95 nM 7.70
CHEMBL4069740 — IC50 = 20.0 nM 7.70
CHEMBL4077184 — IC50 = 21.0 nM 7.68
CHEMBL4105513 — IC50 = 24.0 nM 7.62
CHEMBL4080774 — IC50 = 25.0 nM 7.60
CHEMBL4105513 — IC50 = 25.12 nM 7.60
CHEMBL4080774 — IC50 = 25.12 nM 7.60
CHEMBL4100854 — IC50 = 30.0 nM 7.52
CHEMBL4100854 — IC50 = 31.62 nM 7.50
CHEMBL4096933 — IC50 = 38.0 nM 7.42
CHEMBL4096933 — IC50 = 39.81 nM 7.40
CHEMBL4089231 — IC50 = 50.12 nM 7.30
CHEMBL4086030 — IC50 = 50.12 nM 7.30
CHEMBL4089231 — IC50 = 51.0 nM 7.29
CHEMBL4086030 — IC50 = 52.0 nM 7.28
CHEMBL4070455 — IC50 = 58.0 nM 7.24
CHEMBL4101060 — IC50 = 58.0 nM 7.24
CHEMBL4093788 — IC50 = 60.0 nM 7.22
CHEMBL4101060 — IC50 = 63.1 nM 7.20
CHEMBL4070455 — IC50 = 63.1 nM 7.20
CHEMBL4093788 — IC50 = 63.1 nM 7.20
CHEMBL4101507 — IC50 = 79.43 nM 7.10
CHEMBL4101507 — IC50 = 80.0 nM 7.10
CHEMBL4071465 — IC50 = 79.43 nM 7.10
CHEMBL4071465 — IC50 = 82.0 nM 7.09
CHEMBL4084316 — IC50 = 90.0 nM 7.05
CHEMBL4061058 — IC50 = 90.0 nM 7.05
CHEMBL4082009 — IC50 = 93.0 nM 7.03
CHEMBL4082009 — IC50 = 100.0 nM 7.00