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Assay Detail

CHEMBL1166366

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

Binding
Inhibition of Bacillus thermoproteolyticus thermolysin after 15 mins by microplate fluorescence analysis in presence of 0.1 M substrate FaGLa
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bacillus thermoproteolyticus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Thermolysin (CHEMBL3392)
Type SINGLE PROTEIN
Organism Bacillus thermoproteolyticus

Publication

Identification of novel quinazolin-4(3H)-ones as inhibitors of thermolysin, the prototype of the M4 family of proteinases.
Khan MT, Khan R, Wuxiuer Y, Arfan M, Ahmed M, Sylte I.
Bioorg Med Chem (2010) 18 : 4317 -4327
PubMed 20494587 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 5.37 7.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1164452 1 7.94
CHEMBL1163762 1 6.61
CHEMBL1163173 1 5.90
CHEMBL1163157 1 4.42
CHEMBL1163745 1 4.38
CHEMBL1163152 1 4.26
CHEMBL1164862 1 4.11
CHEMBL1163763 1 -
CHEMBL1164655 1 -
CHEMBL1164451 1 -
CHEMBL1163171 1 -
CHEMBL1165641 1 -
CHEMBL1164444 1 -
CHEMBL1163224 1 -
CHEMBL1163487 1 -
CHEMBL1163483 1 -
CHEMBL1163168 1 -
CHEMBL1163482 1 -
CHEMBL1164448 1 -
CHEMBL1164161 1 -
CHEMBL1164165 1 -
CHEMBL1164078 1 -
CHEMBL1163684 1 -
CHEMBL1163169 1 -
CHEMBL1163683 1 -
CHEMBL1163633 1 -
CHEMBL1163632 1 -
CHEMBL1164450 1 -
CHEMBL1163963 1 -
CHEMBL1163744 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1164452 IC50 = 11.5 nM 7.94
CHEMBL1163762 IC50 = 247.7 nM 6.61
CHEMBL1163173 IC50 = 1250.0 nM 5.90
CHEMBL1163157 IC50 = 37860.0 nM 4.42
CHEMBL1163745 IC50 = 42030.0 nM 4.38
CHEMBL1163152 IC50 = 54890.0 nM 4.26
CHEMBL1164862 IC50 = 76850.0 nM 4.11
CHEMBL1165641 IC50 - -
CHEMBL1163167 IC50 - -
CHEMBL1164444 IC50 - -
CHEMBL1163224 IC50 - -
CHEMBL1163487 IC50 - -
CHEMBL1163483 IC50 - -
CHEMBL1163168 IC50 - -
CHEMBL1163482 IC50 - -
CHEMBL1164655 IC50 = 12743000.0 nM -
CHEMBL1164912 IC50 - -
CHEMBL1164475 IC50 - -
CHEMBL1165543 IC50 - -
CHEMBL1164981 IC50 - -
CHEMBL1164980 IC50 = 3118000.0 nM -
CHEMBL1164861 IC50 - -
CHEMBL1163171 IC50 - -
CHEMBL1164451 IC50 - -
CHEMBL1163763 IC50 - -
CHEMBL1164448 IC50 - -
CHEMBL1164161 IC50 - -
CHEMBL1164165 IC50 - -
CHEMBL1164078 IC50 - -
CHEMBL1163684 IC50 = 122637.0 nM -
CHEMBL1163169 IC50 - -
CHEMBL1163683 IC50 - -
CHEMBL1163633 IC50 - -
CHEMBL1163632 IC50 = 4002000.0 nM -
CHEMBL1164450 IC50 = 1832000.0 nM -
CHEMBL1163963 IC50 - -
CHEMBL1163744 IC50 - -