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Assay Detail

CHEMBL999374

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

Binding
Inhibition of human DPP4 expressed in baculovirus system
26
Total Activities
26
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

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

Publication

A three-dimensional pharmacophore model for dipeptidyl peptidase IV inhibitors.
Lu IL, Tsai KC, Chiang YK, Jiaang WT, Wu SH, Mahindroo N, Chien CH, Lee SJ, Chen X, Chao YS, Wu SY.
Eur J Med Chem (2008) 43 : 1603 -1611
PubMed 18207285 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.91 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL497992 1 8.59
CHEMBL324777 1 8.05
CHEMBL497993 1 7.96
CHEMBL507254 1 7.92
CHEMBL1422 SITAGLIPTIN 4.0 1 7.75
CHEMBL522909 1 7.68
CHEMBL504823 1 7.68
CHEMBL77538 1 7.66
CHEMBL495932 1 7.60
CHEMBL496131 1 7.37
CHEMBL527015 1 7.35
CHEMBL451319 1 7.16
CHEMBL280658 1 7.14
CHEMBL380860 1 6.96
CHEMBL443250 1 6.77
CHEMBL498167 1 6.60
CHEMBL186406 1 6.50
CHEMBL525183 1 6.43
CHEMBL234412 1 6.15
CHEMBL371907 1 5.48
CHEMBL522911 1 4.92
CHEMBL497782 1 4.89
CHEMBL496953 1 4.30
CHEMBL361235 1 -
CHEMBL523066 1 -
CHEMBL509777 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL497992 IC50 = 2.6 nM 8.59
CHEMBL324777 IC50 = 9.0 nM 8.05
CHEMBL497993 IC50 = 11.0 nM 7.96
CHEMBL507254 IC50 = 12.0 nM 7.92
CHEMBL1422 SITAGLIPTIN IC50 = 18.0 nM 7.75
CHEMBL522909 IC50 = 21.0 nM 7.68
CHEMBL504823 IC50 = 21.0 nM 7.68
CHEMBL77538 IC50 = 22.0 nM 7.66
CHEMBL495932 IC50 = 25.0 nM 7.60
CHEMBL496131 IC50 = 43.0 nM 7.37
CHEMBL527015 IC50 = 45.0 nM 7.35
CHEMBL451319 IC50 = 69.0 nM 7.16
CHEMBL280658 IC50 = 73.0 nM 7.14
CHEMBL380860 IC50 = 110.0 nM 6.96
CHEMBL443250 IC50 = 170.0 nM 6.77
CHEMBL498167 IC50 = 250.0 nM 6.60
CHEMBL186406 IC50 = 320.0 nM 6.50
CHEMBL525183 IC50 = 370.0 nM 6.43
CHEMBL234412 IC50 = 710.0 nM 6.15
CHEMBL371907 IC50 = 3300.0 nM 5.48
CHEMBL522911 IC50 = 12000.0 nM 4.92
CHEMBL497782 IC50 = 13000.0 nM 4.89
CHEMBL496953 IC50 = 50000.0 nM 4.30
CHEMBL361235 IC50 = 230000.0 nM -
CHEMBL523066 IC50 = 180000.0 nM -
CHEMBL509777 IC50 = 390000.0 nM -