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Assay Detail

CHEMBL859770

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Binding
Inhibition of DPP4
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors.
Tsai TY, Coumar MS, Hsu T, Hsieh HP, Chien CH, Chen CT, Chang CN, Lo YK, Wu SH, Huang CY, Huang YW, Wang MH, Wu HY, Lee HJ, Chen X, Chao YS, Jiaang WT.
Bioorg Med Chem Lett (2006) 16 : 3268 -3272
PubMed 16581245 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.81 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL210995 1 8.77
CHEMBL201644 1 7.82
CHEMBL208964 1 7.30
CHEMBL209981 1 7.14
CHEMBL210718 1 7.14
CHEMBL210225 1 7.14
CHEMBL210353 1 7.08
CHEMBL379261 1 6.96
CHEMBL427219 1 6.89
CHEMBL377776 1 6.84
CHEMBL378086 1 6.64
CHEMBL210590 1 6.61
CHEMBL210522 1 6.01
CHEMBL210920 1 5.71
CHEMBL210941 1 5.59
CHEMBL380240 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL210995 IC50 = 1.7 nM 8.77
CHEMBL201644 IC50 = 15.0 nM 7.82
CHEMBL208964 IC50 = 50.0 nM 7.30
CHEMBL209981 IC50 = 72.0 nM 7.14
CHEMBL210718 IC50 = 73.0 nM 7.14
CHEMBL210225 IC50 = 73.0 nM 7.14
CHEMBL210353 IC50 = 84.0 nM 7.08
CHEMBL379261 IC50 = 109.0 nM 6.96
CHEMBL427219 IC50 = 129.0 nM 6.89
CHEMBL377776 IC50 = 144.0 nM 6.84
CHEMBL378086 IC50 = 228.0 nM 6.64
CHEMBL210590 IC50 = 245.0 nM 6.61
CHEMBL210522 IC50 = 984.0 nM 6.01
CHEMBL210920 IC50 = 1957.0 nM 5.71
CHEMBL210941 IC50 = 2587.0 nM 5.59
CHEMBL380240 IC50 = 4130.0 nM 5.38