Assay Detail

CHEMBL974348

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Binding

Inhibition of MMP2

ChEMBL ↗

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Target

72 kDa type IV collagenase (CHEMBL333) ↗

Open DB target context

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72 kDa type IV collagenase (CHEMBL333) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target 72 kDa type IV collagenase

CHEMBL333

Anchored from Assay target.

Protein identity 72 kDa type IV collagenase

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

72 kDa type IV collagenase (CHEMBL333) ↗

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	2	9.61	9.70

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL466059	—	—	1	9.70
CHEMBL440498	CTS-1027	2.0	1	9.52

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL466059	—	IC50	=	0.2	nM	9.70
CHEMBL440498	CTS-1027	IC50	=	0.3	nM	9.52