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Assay Detail

CHEMBL938686

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Binding
Inhibition of DPP4
ChEMBL ↗
63
Total Activities
62
Compounds Tested
2
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

Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads.
Van der Veken P, De Meester I, Dubois V, Soroka A, Van Goethem S, Maes MB, Brandt I, Lambeir AM, Chen X, Haemers A, Scharpé S, Augustyns K.
Bioorg Med Chem Lett (2008) 18 : 4154 -4158
PubMed 18556199 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 62 5.19 7.66
Ki 1 4.77 4.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL510594 — — 1 7.66
CHEMBL471544 — — 1 7.46
CHEMBL1422 SITAGLIPTIN 4.0 1 7.40
CHEMBL142703 VILDAGLIPTIN 4.0 2 6.92
CHEMBL471547 — — 1 6.54
CHEMBL461912 — — 1 6.50
CHEMBL471546 — — 1 6.47
CHEMBL471747 — — 1 6.28
CHEMBL472128 — — 1 6.25
CHEMBL98408 — — 1 5.77
CHEMBL471731 — — 1 5.66
CHEMBL518144 — — 1 5.60
CHEMBL460886 — — 1 5.46
CHEMBL461092 — — 1 5.43
CHEMBL453573 — — 1 5.41
CHEMBL503274 — — 1 5.40
CHEMBL383705 — — 1 5.27
CHEMBL460065 — — 1 5.01
CHEMBL461289 — — 1 4.90
CHEMBL403882 — — 1 4.82
CHEMBL442952 — — 1 4.82
CHEMBL461291 — — 1 4.82
CHEMBL459642 — — 1 4.81
CHEMBL461290 — — 1 4.78
CHEMBL98008 — — 1 4.77
CHEMBL453918 — — 1 4.68
CHEMBL501521 — — 1 4.64
CHEMBL455298 — — 1 4.64
CHEMBL453574 — — 1 4.62
CHEMBL459159 — — 1 4.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL510594 — IC50 = 22.0 nM 7.66
CHEMBL471544 — IC50 = 35.0 nM 7.46
CHEMBL1422 SITAGLIPTIN IC50 = 40.0 nM 7.40
CHEMBL142703 VILDAGLIPTIN IC50 = 120.0 nM 6.92
CHEMBL471547 — IC50 = 290.0 nM 6.54
CHEMBL461912 — IC50 = 320.0 nM 6.50
CHEMBL471546 — IC50 = 340.0 nM 6.47
CHEMBL471747 — IC50 = 530.0 nM 6.28
CHEMBL472128 — IC50 = 560.0 nM 6.25
CHEMBL98408 — IC50 = 1700.0 nM 5.77
CHEMBL471731 — IC50 = 2200.0 nM 5.66
CHEMBL518144 — IC50 = 2500.0 nM 5.60
CHEMBL460886 — IC50 = 3500.0 nM 5.46
CHEMBL461092 — IC50 = 3700.0 nM 5.43
CHEMBL453573 — IC50 = 3900.0 nM 5.41
CHEMBL503274 — IC50 = 4000.0 nM 5.40
CHEMBL383705 — IC50 = 5400.0 nM 5.27
CHEMBL460065 — IC50 = 9700.0 nM 5.01
CHEMBL461289 — IC50 = 12700.0 nM 4.90
CHEMBL442952 — IC50 = 15000.0 nM 4.82
CHEMBL461291 — IC50 = 15000.0 nM 4.82
CHEMBL403882 — IC50 = 15000.0 nM 4.82
CHEMBL459642 — IC50 = 15600.0 nM 4.81
CHEMBL461290 — IC50 = 16800.0 nM 4.78
CHEMBL98008 — IC50 = 17000.0 nM 4.77
CHEMBL142703 VILDAGLIPTIN Ki = 17000.0 nM 4.77
CHEMBL453918 — IC50 = 21000.0 nM 4.68
CHEMBL455298 — IC50 = 23000.0 nM 4.64
CHEMBL501521 — IC50 = 23100.0 nM 4.64
CHEMBL453574 — IC50 = 24000.0 nM 4.62
CHEMBL459159 — IC50 = 37000.0 nM 4.43
CHEMBL501126 — IC50 = 39000.0 nM 4.41
CHEMBL443622 — IC50 = 41000.0 nM 4.39
CHEMBL511346 — IC50 = 43500.0 nM 4.36
CHEMBL461496 — IC50 = 50400.0 nM 4.30
CHEMBL461913 — IC50 = 51000.0 nM 4.29
CHEMBL452470 — IC50 = 52000.0 nM 4.28
CHEMBL511659 — IC50 = 52000.0 nM 4.28
CHEMBL83418 — IC50 = 67000.0 nM 4.17
CHEMBL397070 — IC50 = 90000.0 nM 4.05
CHEMBL503809 — IC50 = 93000.0 nM 4.03
CHEMBL460887 — IC50 = 94000.0 nM 4.03
CHEMBL459438 — IC50 = 98000.0 nM 4.01
CHEMBL456298 — IC50 > 1000000.0 nM -
CHEMBL469890 — IC50 = 115000.0 nM -
CHEMBL488226 — IC50 = 161000.0 nM -
CHEMBL97025 — IC50 > 1000000.0 nM -
CHEMBL98869 — IC50 = 165000.0 nM -
CHEMBL449318 — IC50 > 1000000.0 nM -
CHEMBL488227 — IC50 = 245000.0 nM -