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Assay Detail

CHEMBL4018050

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

Binding
Inhibition of recombinant human meprin beta expressed in yeast using Abz-YVAEAPK(Dnp)G-OH as substrate by fluorescence assay
44
Total Activities
44
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

Meprin A subunit beta (CHEMBL4105879)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

First insight into structure-activity relationships of selective meprin β inhibitors.
Ramsbeck D, Hamann A, Schlenzig D, Schilling S, Buchholz M.
Bioorg Med Chem Lett (2017) 27 : 2428 -2431
PubMed 28408220 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 5.41 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4078433 1 7.22
CHEMBL4105563 1 7.22
CHEMBL4099123 1 6.66
CHEMBL4102689 1 6.57
CHEMBL4083600 1 6.51
CHEMBL4087683 1 6.50
CHEMBL4072148 1 6.47
CHEMBL4096428 1 6.40
CHEMBL4101604 1 6.39
CHEMBL4063534 1 6.37
CHEMBL4067530 1 6.19
CHEMBL4083361 1 6.16
CHEMBL4079395 1 6.01
CHEMBL4071300 1 5.97
CHEMBL4098334 1 5.97
CHEMBL4061533 1 5.71
CHEMBL4097429 1 5.59
CHEMBL550148 1 5.42
CHEMBL4064607 1 5.36
CHEMBL4091383 1 5.30
CHEMBL4073192 1 5.25
CHEMBL515083 1 5.22
CHEMBL4085117 1 5.21
CHEMBL4093873 1 5.14
CHEMBL4095310 1 5.13
CHEMBL83508 1 5.04
CHEMBL4084150 1 4.99
CHEMBL4087610 1 4.84
CHEMBL4079737 1 4.83
CHEMBL311932 1 4.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4078433 IC50 = 60.0 nM 7.22
CHEMBL4105563 IC50 = 60.0 nM 7.22
CHEMBL4099123 IC50 = 220.0 nM 6.66
CHEMBL4102689 IC50 = 270.0 nM 6.57
CHEMBL4083600 IC50 = 310.0 nM 6.51
CHEMBL4087683 IC50 = 320.0 nM 6.50
CHEMBL4072148 IC50 = 340.0 nM 6.47
CHEMBL4096428 IC50 = 400.0 nM 6.40
CHEMBL4101604 IC50 = 410.0 nM 6.39
CHEMBL4063534 IC50 = 430.0 nM 6.37
CHEMBL4067530 IC50 = 650.0 nM 6.19
CHEMBL4083361 IC50 = 700.0 nM 6.16
CHEMBL4079395 IC50 = 980.0 nM 6.01
CHEMBL4071300 IC50 = 1080.0 nM 5.97
CHEMBL4098334 IC50 = 1060.0 nM 5.97
CHEMBL4061533 IC50 = 1930.0 nM 5.71
CHEMBL4097429 IC50 = 2550.0 nM 5.59
CHEMBL550148 IC50 = 3850.0 nM 5.42
CHEMBL4064607 IC50 = 4420.0 nM 5.36
CHEMBL4091383 IC50 = 5030.0 nM 5.30
CHEMBL4073192 IC50 = 5650.0 nM 5.25
CHEMBL515083 IC50 = 5980.0 nM 5.22
CHEMBL4085117 IC50 = 6190.0 nM 5.21
CHEMBL4093873 IC50 = 7310.0 nM 5.14
CHEMBL4095310 IC50 = 7420.0 nM 5.13
CHEMBL83508 IC50 = 9020.0 nM 5.04
CHEMBL4084150 IC50 = 10260.0 nM 4.99
CHEMBL4087610 IC50 = 14320.0 nM 4.84
CHEMBL4079737 IC50 = 14770.0 nM 4.83
CHEMBL311932 IC50 = 17100.0 nM 4.77
CHEMBL4066258 IC50 = 17170.0 nM 4.76
CHEMBL4062444 IC50 = 17970.0 nM 4.75
CHEMBL198778 IC50 = 18800.0 nM 4.73
CHEMBL4070398 IC50 = 18850.0 nM 4.72
CHEMBL4103999 IC50 = 25700.0 nM 4.59
CHEMBL4074872 IC50 = 26900.0 nM 4.57
CHEMBL4060490 IC50 = 31200.0 nM 4.51
CHEMBL4088725 IC50 = 32530.0 nM 4.49
CHEMBL82783 IC50 = 34950.0 nM 4.46
CHEMBL4080850 IC50 = 37500.0 nM 4.43
CHEMBL86189 IC50 = 38800.0 nM 4.41
CHEMBL82868 IC50 = 40470.0 nM 4.39
CHEMBL82331 IC50 = 42900.0 nM 4.37
CHEMBL4105128 IC50 = 43870.0 nM 4.36