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Assay Detail

CHEMBL1806089

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

Binding
Inhibition of human MMP13 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay
ChEMBL ↗
45
Total Activities
45
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

Collagenase 3 (CHEMBL280) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
Becker DP, Barta TE, Bedell LJ, Boehm TL, Bond BR, Carroll J, Carron CP, Decrescenzo GA, Easton AM, Freskos JN, Funckes-Shippy CL, Heron M, Hockerman S, Howard CP, Kiefer JR, Li MH, Mathis KJ, McDonald JJ, Mehta PP, Munie GE, Sunyer T, Swearingen CA, Villamil CI, Welsch D, Williams JM, Yu Y, Yao J.
J Med Chem (2010) 53 : 6653 -6680
PubMed 20726512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 9.43 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1801417 — — 1 10.00
CHEMBL1801049 — — 1 10.00
CHEMBL1801429 — — 1 10.00
CHEMBL1801430 — — 1 10.00
CHEMBL1801044 — — 1 10.00
CHEMBL1801046 — — 1 9.82
CHEMBL1801424 — — 1 9.70
CHEMBL1801414 — — 1 9.70
CHEMBL1801421 — — 1 9.70
CHEMBL1801428 — — 1 9.70
CHEMBL1801393 — — 1 9.70
CHEMBL1801396 — — 1 9.70
CHEMBL1801397 — — 1 9.70
CHEMBL1801413 — — 1 9.60
CHEMBL1801050 — — 1 9.60
CHEMBL1801412 — — 1 9.60
CHEMBL1801054 — — 1 9.60
CHEMBL1801057 — — 1 9.52
CHEMBL1801422 — — 1 9.52
CHEMBL1801048 — — 1 9.52
CHEMBL1800089 — — 1 9.46
CHEMBL1082381 — — 1 9.40
CHEMBL1229868 — — 1 9.40
CHEMBL1801056 — — 1 9.40
CHEMBL1801045 — — 1 9.35
CHEMBL1801416 — — 1 9.30
CHEMBL1801423 — — 1 9.30
CHEMBL1801420 — — 1 9.22
CHEMBL1801398 — — 1 9.22
CHEMBL1801427 — — 1 9.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1801417 — IC50 = 0.1 nM 10.00
CHEMBL1801044 — IC50 = 0.1 nM 10.00
CHEMBL1801430 — IC50 = 0.1 nM 10.00
CHEMBL1801049 — IC50 = 0.1 nM 10.00
CHEMBL1801429 — IC50 = 0.1 nM 10.00
CHEMBL1801046 — IC50 = 0.15 nM 9.82
CHEMBL1801424 — IC50 = 0.2 nM 9.70
CHEMBL1801414 — IC50 = 0.2 nM 9.70
CHEMBL1801421 — IC50 = 0.2 nM 9.70
CHEMBL1801428 — IC50 = 0.2 nM 9.70
CHEMBL1801393 — IC50 = 0.2 nM 9.70
CHEMBL1801396 — IC50 = 0.2 nM 9.70
CHEMBL1801397 — IC50 = 0.2 nM 9.70
CHEMBL1801054 — IC50 = 0.25 nM 9.60
CHEMBL1801050 — IC50 = 0.25 nM 9.60
CHEMBL1801413 — IC50 = 0.25 nM 9.60
CHEMBL1801412 — IC50 = 0.25 nM 9.60
CHEMBL1801057 — IC50 = 0.3 nM 9.52
CHEMBL1801422 — IC50 = 0.3 nM 9.52
CHEMBL1801048 — IC50 = 0.3 nM 9.52
CHEMBL1800089 — IC50 = 0.35 nM 9.46
CHEMBL1801056 — IC50 = 0.4 nM 9.40
CHEMBL1229868 — IC50 = 0.4 nM 9.40
CHEMBL1082381 — IC50 = 0.4 nM 9.40
CHEMBL1801045 — IC50 = 0.45 nM 9.35
CHEMBL1801416 — IC50 = 0.5 nM 9.30
CHEMBL1801423 — IC50 = 0.5 nM 9.30
CHEMBL1801420 — IC50 = 0.6 nM 9.22
CHEMBL1801398 — IC50 = 0.6 nM 9.22
CHEMBL1801427 — IC50 = 0.6 nM 9.22
CHEMBL1801051 — IC50 = 0.8 nM 9.10
CHEMBL1801047 — IC50 = 0.8 nM 9.10
CHEMBL1801055 — IC50 = 1.0 nM 9.00
CHEMBL1801425 — IC50 = 1.2 nM 8.92
CHEMBL1801419 — IC50 = 1.9 nM 8.72
CHEMBL1801415 — IC50 = 2.7 nM 8.57
CHEMBL1801418 — IC50 = 2.9 nM 8.54
CHEMBL1801426 — IC50 = 5.5 nM 8.26
CHEMBL1801052 — IC50 < 0.1 nM -
CHEMBL1801053 — IC50 < 0.1 nM -
CHEMBL1771212 — IC50 < 0.1 nM -
CHEMBL1801431 — IC50 < 0.1 nM -
CHEMBL1801394 — IC50 < 0.1 nM -
CHEMBL1801395 — IC50 < 0.1 nM -
CHEMBL1801399 — IC50 < 0.1 nM -