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Assay Detail

CHEMBL1058857

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Binding
Inhibition of DPP4 by continuous fluorimetric assay
23
Total Activities
23
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

Discovery of beta-homophenylalanine based pyrrolidin-2-ylmethyl amides and sulfonamides as highly potent and selective inhibitors of dipeptidyl peptidase IV.
Nordhoff S, Cerezo-Gálvez S, Deppe H, Hill O, López-Canet M, Rummey C, Thiemann M, Matassa VG, Edwards PJ, Feurer A.
Bioorg Med Chem Lett (2009) 19 : 4201 -4203
PubMed 19515557 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.56 9.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL564249 1 9.42
CHEMBL563272 1 8.10
CHEMBL561322 1 8.10
CHEMBL563648 1 8.05
CHEMBL561120 1 7.92
CHEMBL564043 1 7.85
CHEMBL549432 1 7.70
CHEMBL560183 1 7.62
CHEMBL565056 1 7.57
CHEMBL562525 1 7.57
CHEMBL563108 1 7.57
CHEMBL560184 1 7.52
CHEMBL539187 1 7.47
CHEMBL560123 1 7.33
CHEMBL550862 1 7.31
CHEMBL549842 1 7.28
CHEMBL562981 1 7.18
CHEMBL557851 1 7.11
CHEMBL563911 1 7.06
CHEMBL425584 1 7.05
CHEMBL553936 1 7.04
CHEMBL552263 1 7.04
CHEMBL562603 1 7.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL564249 IC50 = 0.38 nM 9.42
CHEMBL563272 IC50 = 8.0 nM 8.10
CHEMBL561322 IC50 = 8.0 nM 8.10
CHEMBL563648 IC50 = 9.0 nM 8.05
CHEMBL561120 IC50 = 12.0 nM 7.92
CHEMBL564043 IC50 = 14.0 nM 7.85
CHEMBL549432 IC50 = 20.0 nM 7.70
CHEMBL560183 IC50 = 24.0 nM 7.62
CHEMBL565056 IC50 = 27.0 nM 7.57
CHEMBL562525 IC50 = 27.0 nM 7.57
CHEMBL563108 IC50 = 27.0 nM 7.57
CHEMBL560184 IC50 = 30.0 nM 7.52
CHEMBL539187 IC50 = 34.0 nM 7.47
CHEMBL560123 IC50 = 47.0 nM 7.33
CHEMBL550862 IC50 = 49.0 nM 7.31
CHEMBL549842 IC50 = 53.0 nM 7.28
CHEMBL562981 IC50 = 66.0 nM 7.18
CHEMBL557851 IC50 = 77.0 nM 7.11
CHEMBL563911 IC50 = 87.0 nM 7.06
CHEMBL425584 IC50 = 90.0 nM 7.05
CHEMBL553936 IC50 = 92.0 nM 7.04
CHEMBL552263 IC50 = 92.0 nM 7.04
CHEMBL562603 IC50 = 94.0 nM 7.03