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Assay Detail

CHEMBL886679

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Binding
Inhibition of DPP4 in rat plasma by fluorescence assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Plasma
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Dipeptidyl peptidase 4 (CHEMBL4653)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

[(S)-gamma-(4-Aryl-1-piperazinyl)-l-prolyl]thiazolidines as a novel series of highly potent and long-lasting DPP-IV inhibitors.
Yoshida T, Sakashita H, Akahoshi F, Hayashi Y.
Bioorg Med Chem Lett (2007) 17 : 2618 -2621
PubMed 17317162 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 8.08 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL399610 1 8.96
CHEMBL241464 1 8.92
CHEMBL241253 1 8.85
CHEMBL241252 1 8.74
CHEMBL238515 1 8.74
CHEMBL399405 1 8.72
CHEMBL391466 1 8.66
CHEMBL239356 1 8.54
CHEMBL239565 1 8.51
CHEMBL238516 1 8.48
CHEMBL395854 1 8.46
CHEMBL239564 1 8.41
CHEMBL241246 1 8.38
CHEMBL391578 1 8.33
CHEMBL391577 1 8.14
CHEMBL241245 1 8.14
CHEMBL239984 1 8.05
CHEMBL395606 1 8.02
CHEMBL238507 1 7.99
CHEMBL239983 1 7.96
CHEMBL238506 1 7.77
CHEMBL397893 1 7.76
CHEMBL240601 1 7.75
CHEMBL241674 1 7.72
CHEMBL240602 1 7.50
CHEMBL391433 1 7.42
CHEMBL391331 1 7.13
CHEMBL391332 1 7.09
CHEMBL241673 1 6.92
CHEMBL224435 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL399610 IC50 = 1.1 nM 8.96
CHEMBL241464 IC50 = 1.2 nM 8.92
CHEMBL241253 IC50 = 1.4 nM 8.85
CHEMBL241252 IC50 = 1.8 nM 8.74
CHEMBL238515 IC50 = 1.8 nM 8.74
CHEMBL399405 IC50 = 1.9 nM 8.72
CHEMBL391466 IC50 = 2.2 nM 8.66
CHEMBL239356 IC50 = 2.9 nM 8.54
CHEMBL239565 IC50 = 3.1 nM 8.51
CHEMBL238516 IC50 = 3.3 nM 8.48
CHEMBL395854 IC50 = 3.5 nM 8.46
CHEMBL239564 IC50 = 3.9 nM 8.41
CHEMBL241246 IC50 = 4.2 nM 8.38
CHEMBL391578 IC50 = 4.7 nM 8.33
CHEMBL391577 IC50 = 7.2 nM 8.14
CHEMBL241245 IC50 = 7.2 nM 8.14
CHEMBL239984 IC50 = 9.0 nM 8.05
CHEMBL395606 IC50 = 9.6 nM 8.02
CHEMBL238507 IC50 = 10.3 nM 7.99
CHEMBL239983 IC50 = 10.9 nM 7.96
CHEMBL238506 IC50 = 16.9 nM 7.77
CHEMBL397893 IC50 = 17.5 nM 7.76
CHEMBL240601 IC50 = 17.6 nM 7.75
CHEMBL241674 IC50 = 18.9 nM 7.72
CHEMBL240602 IC50 = 31.4 nM 7.50
CHEMBL391433 IC50 = 38.3 nM 7.42
CHEMBL391331 IC50 = 74.4 nM 7.13
CHEMBL391332 IC50 = 81.1 nM 7.09
CHEMBL241673 IC50 = 121.0 nM 6.92
CHEMBL224435 IC50 = 607.0 nM 6.22