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Assay Detail

CHEMBL1955693

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

Binding
Inhibition of human recombinant PrCP using Mca-Ala-Pro-Lys(Dnp)-OH as substrate for 30 mins by continuous fluorimetric assay
25
Total Activities
25
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 of a new class of potent prolylcarboxypeptidase inhibitors derived from alanine.
Wu Z, Yang C, Xiong Y, Feng Z, Lombardo M, Verras A, Chabin RM, Xu S, Tong X, Xie D, Lassman ME, Bhatt UR, Garcia-Calvo MM, Geissler W, Shen Z, Chen Q, Sinharoy R, Hale JJ, Tata JR, Pinto S, Shen DM, Colletti SL.
Bioorg Med Chem Lett (2012) 22 : 1774 -1778
PubMed 22248857 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.73 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1950440 1 9.77
CHEMBL1950444 1 9.43
CHEMBL1950439 1 9.13
CHEMBL1950443 1 9.00
CHEMBL1950445 1 8.59
CHEMBL1950309 1 8.30
CHEMBL1950314 1 8.25
CHEMBL1950441 1 8.18
CHEMBL1950307 1 8.00
CHEMBL1950311 1 7.85
CHEMBL1950310 1 7.80
CHEMBL1950308 1 7.42
CHEMBL1950448 1 7.32
CHEMBL1950451 1 7.22
CHEMBL1950442 1 6.99
CHEMBL1950446 1 6.80
CHEMBL1950312 1 6.74
CHEMBL1950449 1 6.65
CHEMBL1950450 1 6.43
CHEMBL1950313 1 6.37
CHEMBL1950447 1 6.00
CHEMBL1950452 1 -
CHEMBL1950453 1 -
CHEMBL1950454 1 -
CHEMBL1950455 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1950440 IC50 = 0.17 nM 9.77
CHEMBL1950444 IC50 = 0.37 nM 9.43
CHEMBL1950439 IC50 = 0.74 nM 9.13
CHEMBL1950443 IC50 = 1.0 nM 9.00
CHEMBL1950445 IC50 = 2.6 nM 8.59
CHEMBL1950309 IC50 = 5.0 nM 8.30
CHEMBL1950314 IC50 = 5.6 nM 8.25
CHEMBL1950441 IC50 = 6.6 nM 8.18
CHEMBL1950307 IC50 = 10.0 nM 8.00
CHEMBL1950311 IC50 = 14.0 nM 7.85
CHEMBL1950310 IC50 = 16.0 nM 7.80
CHEMBL1950308 IC50 = 38.0 nM 7.42
CHEMBL1950448 IC50 = 48.0 nM 7.32
CHEMBL1950451 IC50 = 60.0 nM 7.22
CHEMBL1950442 IC50 = 102.0 nM 6.99
CHEMBL1950446 IC50 = 160.0 nM 6.80
CHEMBL1950312 IC50 = 181.0 nM 6.74
CHEMBL1950449 IC50 = 225.0 nM 6.65
CHEMBL1950450 IC50 = 374.0 nM 6.43
CHEMBL1950313 IC50 = 427.0 nM 6.37
CHEMBL1950447 IC50 = 998.0 nM 6.00
CHEMBL1950452 IC50 > 10000.0 nM -
CHEMBL1950453 IC50 > 10000.0 nM -
CHEMBL1950454 IC50 > 10000.0 nM -
CHEMBL1950455 IC50 > 10000.0 nM -