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Assay Detail

CHEMBL3090541

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

Functional
Ex-vivo inhibition of PrCP in plasma of po dosed C57 mouse after 20 hrs by FRET analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Tissue Plasma
Confidence 1 — Organism
Curated By Autocuration

Target

Mus musculus (CHEMBL375)
Type ORGANISM
Organism Mus musculus

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
Ki 4 7.66 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3086040 1 8.96
CHEMBL3086028 1 7.72
CHEMBL3086036 1 7.15
CHEMBL3086041 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3086040 Ki = 1.1 nM 8.96
CHEMBL3086028 Ki = 19.0 nM 7.72
CHEMBL3086036 Ki = 70.5 nM 7.15
CHEMBL3086041 Ki = 158.0 nM 6.80