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Assay Detail

CHEMBL896429

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

Binding
Inhibition of DPP4
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Dipeptidyl peptidase 4 (CHEMBL284)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Modeling assisted rational design of novel, potent, and selective pyrrolopyrimidine DPP-4 inhibitors.
Gao YD, Feng D, Sheridan RP, Scapin G, Patel SB, Wu JK, Zhang X, Sinha-Roy R, Thornberry NA, Weber AE, Biftu T.
Bioorg Med Chem Lett (2007) 17 : 3877 -3879
PubMed 17502141 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.21 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL233564 1 9.17
CHEMBL233563 1 8.28
CHEMBL392924 1 8.18
CHEMBL1422 SITAGLIPTIN 4.0 1 7.75
CHEMBL233360 1 7.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL233564 IC50 = 0.67 nM 9.17
CHEMBL233563 IC50 = 5.3 nM 8.28
CHEMBL392924 IC50 = 6.6 nM 8.18
CHEMBL1422 SITAGLIPTIN IC50 = 18.0 nM 7.75
CHEMBL233360 IC50 = 21.0 nM 7.68