Assay Detail

CHEMBL974353

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Binding

Inhibition of TACE

ChEMBL ↗

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Target

Disintegrin and metalloproteinase domain-containing protein 17 (CHEMBL3706) ↗

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Disintegrin and metalloproteinase domain-containing protein 17 (CHEMBL3706) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Disintegrin and metalloproteinase domain-containing protein 17

CHEMBL3706

Anchored from Assay target.

Protein identity Disintegrin and metalloproteinase domain-containing protein 17

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Confidence	8 — Homologous single protein target
Curated By	Intermediate

Target

Disintegrin and metalloproteinase domain-containing protein 17 (CHEMBL3706) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.

Monovich LG, Tommasi RA, Fujimoto RA, Blancuzzi V, Clark K, Cornell WD, Doti R, Doughty J, Fang J, Farley D, Fitt J, Ganu V, Goldberg R, Goldstein R, Lavoie S, Kulathila R, Macchia W, Parker DT, Melton R, O'Byrne E, Pastor G, Pellas T, Quadros E, Reel N, Roland DM, Sakane Y, Singh H, Skiles J, Somers J, Toscano K, Wigg A, Zhou S, Zhu L, Shieh WC, Xue S, McQuire LW.
J Med Chem (2009) 52 : 3523 -3538
PubMed 19422229 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	4	6.80	7.39

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL514138	CGS-27023A	—	1	7.39
CHEMBL115653	CIPEMASTAT	2.0	1	6.64
CHEMBL440498	CTS-1027	2.0	1	6.36
CHEMBL466059	—	—	1	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL514138	CGS-27023A	IC50	=	40.9	nM	7.39
CHEMBL115653	CIPEMASTAT	IC50	=	230.3	nM	6.64
CHEMBL440498	CTS-1027	IC50	=	440.0	nM	6.36
CHEMBL466059	—	IC50	>	1000.0	nM	-