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Assay Detail

CHEMBL974341

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Binding
Inhibition of MMP1
54
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Interstitial collagenase (CHEMBL332)
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 54 5.81 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL115653 CIPEMASTAT 2.0 1 8.64
CHEMBL514138 CGS-27023A 1 7.38
CHEMBL440498 CTS-1027 2.0 1 6.45
CHEMBL494823 1 6.19
CHEMBL468739 1 6.17
CHEMBL466052 1 6.11
CHEMBL499159 1 6.02
CHEMBL512237 1 5.89
CHEMBL466237 1 5.76
CHEMBL467459 1 5.70
CHEMBL493177 1 5.64
CHEMBL468738 1 5.49
CHEMBL512061 1 5.47
CHEMBL511729 1 5.44
CHEMBL493178 1 5.38
CHEMBL493989 1 5.37
CHEMBL466059 1 5.34
CHEMBL467460 1 5.20
CHEMBL466249 1 5.18
CHEMBL468731 1 5.15
CHEMBL512275 1 5.03
CHEMBL494824 1 4.89
CHEMBL466060 1 -
CHEMBL466461 1 -
CHEMBL513823 1 -
CHEMBL512613 1 -
CHEMBL466208 1 -
CHEMBL466045 1 -
CHEMBL466656 1 -
CHEMBL466657 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL115653 CIPEMASTAT IC50 = 2.3 nM 8.64
CHEMBL514138 CGS-27023A IC50 = 42.0 nM 7.38
CHEMBL440498 CTS-1027 IC50 = 356.0 nM 6.45
CHEMBL494823 IC50 = 650.0 nM 6.19
CHEMBL468739 IC50 = 680.0 nM 6.17
CHEMBL466052 IC50 = 770.0 nM 6.11
CHEMBL499159 IC50 = 950.0 nM 6.02
CHEMBL512237 IC50 = 1290.0 nM 5.89
CHEMBL466237 IC50 = 1740.0 nM 5.76
CHEMBL467459 IC50 = 2020.0 nM 5.70
CHEMBL493177 IC50 = 2300.0 nM 5.64
CHEMBL468738 IC50 = 3230.0 nM 5.49
CHEMBL512061 IC50 = 3350.0 nM 5.47
CHEMBL511729 IC50 = 3600.0 nM 5.44
CHEMBL493178 IC50 = 4180.0 nM 5.38
CHEMBL493989 IC50 = 4300.0 nM 5.37
CHEMBL466059 IC50 = 4540.0 nM 5.34
CHEMBL467460 IC50 = 6370.0 nM 5.20
CHEMBL466249 IC50 = 6560.0 nM 5.18
CHEMBL468731 IC50 = 7050.0 nM 5.15
CHEMBL512275 IC50 = 9330.0 nM 5.03
CHEMBL494824 IC50 = 12900.0 nM 4.89
CHEMBL513148 IC50 - -
CHEMBL494167 IC50 > 10000.0 nM -
CHEMBL466024 IC50 > 10000.0 nM -
CHEMBL511433 IC50 > 10000.0 nM -
CHEMBL469138 IC50 > 10000.0 nM -
CHEMBL467262 IC50 > 10000.0 nM -
CHEMBL468096 IC50 > 10000.0 nM -
CHEMBL493179 IC50 > 10000.0 nM -
CHEMBL492383 IC50 > 10000.0 nM -
CHEMBL492384 IC50 > 10000.0 nM -
CHEMBL466460 IC50 > 10000.0 nM -
CHEMBL468095 IC50 > 10000.0 nM -
CHEMBL467687 IC50 > 10000.0 nM -
CHEMBL467482 IC50 > 10000.0 nM -
CHEMBL468737 IC50 > 10000.0 nM -
CHEMBL466625 IC50 > 10000.0 nM -
CHEMBL513822 IC50 > 10000.0 nM -
CHEMBL468708 IC50 > 10000.0 nM -
CHEMBL466664 IC50 > 10000.0 nM -
CHEMBL466663 IC50 > 10000.0 nM -
CHEMBL466657 IC50 > 10000.0 nM -
CHEMBL466656 IC50 > 10000.0 nM -
CHEMBL466045 IC50 > 10000.0 nM -
CHEMBL466208 IC50 > 10000.0 nM -
CHEMBL512613 IC50 > 10000.0 nM -
CHEMBL513823 IC50 > 10000.0 nM -
CHEMBL466461 IC50 > 10000.0 nM -
CHEMBL466060 IC50 > 10000.0 nM -