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Assay Detail

CHEMBL3090540

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

Binding
Inhibition of recombinant human PrCP using Mca-Ala-Pro-Lys(Dnp)-OH as substrate measured for 30 mins by fluorescence assay
24
Total Activities
22
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

Lysosomal Pro-X carboxypeptidase (CHEMBL2335)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors.
Debenham JS, Graham TH, Verras A, Zhang Y, Clements MJ, Kuethe JT, Madsen-Duggan C, Liu W, Bhatt UR, Chen D, Chen Q, Garcia-Calvo M, Geissler WM, He H, Li X, Lisnock J, Shen Z, Tong X, Tung EC, Wiltsie J, Xu S, Hale JJ, Pinto S, Shen DM.
Bioorg Med Chem Lett (2013) 23 : 6228 -6233
PubMed 24157366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 8.09 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3086040 1 10.10
CHEMBL3086037 1 9.74
CHEMBL3085780 1 9.22
CHEMBL3086036 1 9.18
CHEMBL3086041 1 9.02
CHEMBL3086029 1 8.92
CHEMBL3086038 1 8.66
CHEMBL3086048 1 8.60
CHEMBL3086045 2 8.60
CHEMBL3086035 1 8.59
CHEMBL3086039 1 8.57
CHEMBL3086034 1 8.52
CHEMBL3086042 1 8.34
CHEMBL3086032 1 7.92
CHEMBL3086028 1 7.78
CHEMBL3086030 1 7.77
CHEMBL3086047 1 7.54
CHEMBL3086043 1 7.44
CHEMBL3086046 2 7.37
CHEMBL3086044 1 6.70
CHEMBL3086031 1 6.36
CHEMBL3086033 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3086040 IC50 = 0.079 nM 10.10
CHEMBL3086037 IC50 = 0.18 nM 9.74
CHEMBL3085780 IC50 = 0.6 nM 9.22
CHEMBL3086036 IC50 = 0.66 nM 9.18
CHEMBL3086041 IC50 = 0.95 nM 9.02
CHEMBL3086029 IC50 = 1.2 nM 8.92
CHEMBL3086038 IC50 = 2.2 nM 8.66
CHEMBL3086048 IC50 = 2.5 nM 8.60
CHEMBL3086045 IC50 = 2.5 nM 8.60
CHEMBL3086035 IC50 = 2.6 nM 8.59
CHEMBL3086039 IC50 = 2.7 nM 8.57
CHEMBL3086034 IC50 = 3.0 nM 8.52
CHEMBL3086042 IC50 = 4.6 nM 8.34
CHEMBL3086032 IC50 = 12.0 nM 7.92
CHEMBL3086028 IC50 = 16.7 nM 7.78
CHEMBL3086030 IC50 = 17.0 nM 7.77
CHEMBL3086047 IC50 = 29.0 nM 7.54
CHEMBL3086043 IC50 = 36.0 nM 7.44
CHEMBL3086046 IC50 = 43.0 nM 7.37
CHEMBL3086045 IC50 = 192.0 nM 6.72
CHEMBL3086044 IC50 = 198.0 nM 6.70
CHEMBL3086031 IC50 = 440.0 nM 6.36
CHEMBL3086033 IC50 = 480.0 nM 6.32
CHEMBL3086046 IC50 = 642.0 nM 6.19