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Assay Detail

CHEMBL1932594

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

Binding
Inhibition of human recombinant FAP expressed in baculovirus-infected Sf9 insect cells using H-Ala-Pro-AFC as substrate after 60 mins by fluorescence assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prolyl endopeptidase FAP (CHEMBL4683)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and pharmacological characterization of N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor.
Kato N, Oka M, Murase T, Yoshida M, Sakairi M, Yamashita S, Yasuda Y, Yoshikawa A, Hayashi Y, Makino M, Takeda M, Mirensha Y, Kakigami T.
Bioorg Med Chem (2011) 19 : 7221 -7227
PubMed 22019046 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.14 4.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1929396 ANAGLIPTIN 4.0 1 4.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1929396 ANAGLIPTIN IC50 = 72700.0 nM 4.14