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Assay Detail

CHEMBL915601

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Binding
Inhibition of human recombinant DPP8
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dipeptidyl peptidase 8 (CHEMBL4657)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Lead optimization of [(S)-gamma-(arylamino)prolyl]thiazolidine focused on gamma-substituent: Indoline compounds as potent DPP-IV inhibitors.
Sakashita H, Akahoshi F, Yoshida T, Kitajima H, Hayashi Y, Ishii S, Takashina Y, Tsutsumiuchi R, Ono S.
Bioorg Med Chem (2007) 15 : 641 -655
PubMed 17113301 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.94 6.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388111 1 6.42
CHEMBL223914 1 6.25
CHEMBL223497 1 6.17
CHEMBL389244 1 6.13
CHEMBL224435 1 5.33
CHEMBL390513 1 5.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388111 IC50 = 378.8 nM 6.42
CHEMBL223914 IC50 = 562.8 nM 6.25
CHEMBL223497 IC50 = 678.9 nM 6.17
CHEMBL389244 IC50 = 736.5 nM 6.13
CHEMBL224435 IC50 = 4687.0 nM 5.33
CHEMBL390513 IC50 = 4756.0 nM 5.32