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Assay Detail

CHEMBL5381507

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

Binding
Inhibition of recombinant human PEPD using Ala-Pro as substrate assessed as alanine release by measuring increase in fluorescense signal by fluorescence based analysis
48
Total Activities
48
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Xaa-Pro dipeptidase (CHEMBL4185)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimized M24B Aminopeptidase Inhibitors for CARD8 Inflammasome Activation.
Chen Q, Wang A, Covelli DJ, Bhattacharjee A, Wang Q, Orth-He EL, Rao SD, Huang HC, Ball DP, Hsiao JC, Bachovchin DA.
J Med Chem (2023) 66 : 2589 -2607
PubMed 36724486 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 5.59 6.55
Inhibition 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5419166 1 6.55
CHEMBL5433567 1 6.54
CHEMBL5435351 1 6.52
CHEMBL5429139 1 6.28
CHEMBL5433668 1 6.25
CHEMBL5437413 1 6.17
CHEMBL5419034 1 6.14
CHEMBL5393876 1 6.14
CHEMBL5401781 1 6.08
CHEMBL5407130 1 6.08
CHEMBL5410658 1 6.04
CHEMBL5403940 1 6.00
CHEMBL5399924 1 5.92
CHEMBL5396150 1 5.89
CHEMBL5438777 1 5.82
CHEMBL5436435 1 5.82
CHEMBL5396773 1 5.80
CHEMBL5398054 1 5.77
CHEMBL5421036 1 5.75
CHEMBL5394915 1 5.75
CHEMBL5404330 1 5.70
CHEMBL5433606 1 5.66
CHEMBL5406619 1 5.55
CHEMBL5419938 1 5.43
CHEMBL5430934 1 5.40
CHEMBL5403929 1 5.38
CHEMBL5400780 1 5.24
CHEMBL5432938 1 5.21
CHEMBL5403681 1 5.12
CHEMBL5403523 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5419166 IC50 = 280.0 nM 6.55
CHEMBL5433567 IC50 = 290.0 nM 6.54
CHEMBL5435351 IC50 = 300.0 nM 6.52
CHEMBL5429139 IC50 = 530.0 nM 6.28
CHEMBL5433668 IC50 = 560.0 nM 6.25
CHEMBL5437413 IC50 = 670.0 nM 6.17
CHEMBL5419034 IC50 = 720.0 nM 6.14
CHEMBL5393876 IC50 = 720.0 nM 6.14
CHEMBL5401781 IC50 = 840.0 nM 6.08
CHEMBL5407130 IC50 = 840.0 nM 6.08
CHEMBL5410658 IC50 = 910.0 nM 6.04
CHEMBL5403940 IC50 = 1000.0 nM 6.00
CHEMBL5399924 IC50 = 1200.0 nM 5.92
CHEMBL5396150 IC50 = 1300.0 nM 5.89
CHEMBL5436435 IC50 = 1500.0 nM 5.82
CHEMBL5438777 IC50 = 1500.0 nM 5.82
CHEMBL5396773 IC50 = 1600.0 nM 5.80
CHEMBL5398054 IC50 = 1700.0 nM 5.77
CHEMBL5421036 IC50 = 1800.0 nM 5.75
CHEMBL5394915 IC50 = 1800.0 nM 5.75
CHEMBL5404330 IC50 = 2000.0 nM 5.70
CHEMBL5433606 IC50 = 2200.0 nM 5.66
CHEMBL5406619 IC50 = 2800.0 nM 5.55
CHEMBL5419938 IC50 = 3700.0 nM 5.43
CHEMBL5430934 IC50 = 4000.0 nM 5.40
CHEMBL5403929 IC50 = 4200.0 nM 5.38
CHEMBL5400780 IC50 = 5700.0 nM 5.24
CHEMBL5432938 IC50 = 6200.0 nM 5.21
CHEMBL5403681 IC50 = 7600.0 nM 5.12
CHEMBL5403523 IC50 = 7500.0 nM 5.12
CHEMBL5438224 IC50 = 7600.0 nM 5.12
CHEMBL5402862 IC50 = 10000.0 nM 5.00
CHEMBL5435178 IC50 = 11000.0 nM 4.96
CHEMBL5409645 IC50 = 12000.0 nM 4.92
CHEMBL5419889 IC50 = 14000.0 nM 4.85
CHEMBL5397935 IC50 = 14000.0 nM 4.85
CHEMBL311875 IC50 = 26000.0 nM 4.58
CHEMBL5415840 IC50 = 51000.0 nM 4.29
CHEMBL5427035 IC50 = 66000.0 nM 4.18
CHEMBL5424113 Inhibition - % -
CHEMBL5408940 Inhibition - % -
CHEMBL5426465 Inhibition - % -
CHEMBL67279 TALABOSTAT IC50 ~ 10000.0 nM -
CHEMBL5412812 IC50 > 100000.0 nM -
CHEMBL5421582 IC50 > 100000.0 nM -
CHEMBL5415378 IC50 > 100000.0 nM -
CHEMBL457092 BESTATIN METHYL ESTER IC50 > 100000.0 nM -
CHEMBL5412099 IC50 > 100000.0 nM -