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Assay Detail

CHEMBL4688202

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

Binding
Inhibition of GST-tagged Pin1 (unknown origin) using Suc-Ala-pSer-Pro-Phe-pNA as substrate preincubated with enzyme for 12 hrs followed by substrate addition by chymotrypsin coupled assay
2
Total Activities
2
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

Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (CHEMBL2288)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of novel thiazole-based derivatives as human Pin1 inhibitors.
Du L,Wang X,Cui G,Xu B
Bioorg Med Chem (2021) 29 : 115878 -115878
PubMed 33246256 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.51 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4751817 1 7.70
CHEMBL4750217 1 7.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4751817 Ki = 20.0 nM 7.70
CHEMBL4750217 Ki = 48.0 nM 7.32