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Assay Detail

CHEMBL1119677

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

Binding
Inhibition of DPP4
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
Yeh TK, Tsai TY, Hsu T, Cheng JH, Chen X, Song JS, Shy HS, Chiou MC, Chien CH, Tseng YJ, Huang CY, Yeh KC, Huang YL, Huang CH, Huang YW, Wang MH, Tang HK, Chao YS, Chen CT, Jiaang WT.
Bioorg Med Chem Lett (2010) 20 : 3596 -3600
PubMed 20483603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.48 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL385517 SAXAGLIPTIN ANHYDROUS 4.0 1 8.47
CHEMBL1082462 DBPR-108 3.0 1 7.82
CHEMBL201644 1 7.82
CHEMBL1082996 1 7.82
CHEMBL1085075 1 7.75
CHEMBL1085306 1 7.72
CHEMBL1085552 1 7.72
CHEMBL1085333 1 7.70
CHEMBL1085595 1 7.62
CHEMBL1086039 1 7.62
CHEMBL1085332 1 7.58
CHEMBL1085074 1 7.57
CHEMBL1085580 1 7.57
CHEMBL1085305 1 7.57
CHEMBL1084972 1 7.54
CHEMBL1422 SITAGLIPTIN 4.0 1 7.52
CHEMBL1082463 1 7.52
CHEMBL1085579 1 7.50
CHEMBL1082465 1 7.41
CHEMBL1082464 1 7.30
CHEMBL142703 VILDAGLIPTIN 4.0 1 7.29
CHEMBL1085597 1 7.20
CHEMBL1084601 1 7.18
CHEMBL1082997 1 7.15
CHEMBL1085596 1 7.03
CHEMBL217198 1 6.94
CHEMBL1085598 1 6.80
CHEMBL1086502 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL385517 SAXAGLIPTIN ANHYDROUS IC50 = 3.4 nM 8.47
CHEMBL1082462 DBPR-108 IC50 = 15.0 nM 7.82
CHEMBL201644 IC50 = 15.0 nM 7.82
CHEMBL1082996 IC50 = 15.0 nM 7.82
CHEMBL1085075 IC50 = 18.0 nM 7.75
CHEMBL1085306 IC50 = 19.0 nM 7.72
CHEMBL1085552 IC50 = 19.0 nM 7.72
CHEMBL1085333 IC50 = 20.0 nM 7.70
CHEMBL1085595 IC50 = 24.0 nM 7.62
CHEMBL1086039 IC50 = 24.0 nM 7.62
CHEMBL1085332 IC50 = 26.0 nM 7.58
CHEMBL1085074 IC50 = 27.0 nM 7.57
CHEMBL1085580 IC50 = 27.0 nM 7.57
CHEMBL1085305 IC50 = 27.0 nM 7.57
CHEMBL1084972 IC50 = 29.0 nM 7.54
CHEMBL1422 SITAGLIPTIN IC50 = 30.0 nM 7.52
CHEMBL1082463 IC50 = 30.0 nM 7.52
CHEMBL1085579 IC50 = 32.0 nM 7.50
CHEMBL1082465 IC50 = 39.0 nM 7.41
CHEMBL1082464 IC50 = 50.0 nM 7.30
CHEMBL142703 VILDAGLIPTIN IC50 = 51.0 nM 7.29
CHEMBL1085597 IC50 = 63.0 nM 7.20
CHEMBL1084601 IC50 = 66.0 nM 7.18
CHEMBL1082997 IC50 = 71.0 nM 7.15
CHEMBL1085596 IC50 = 93.0 nM 7.03
CHEMBL217198 IC50 = 116.0 nM 6.94
CHEMBL1085598 IC50 = 160.0 nM 6.80
CHEMBL1086502 IC50 = 180.0 nM 6.75