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Assay Detail

CHEMBL665782

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

Binding
In vitro inhibition of porcine Dipeptidylpeptidase IV.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dipeptidyl peptidase 4 (CHEMBL3813)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Synthesis of novel potent dipeptidyl peptidase IV inhibitors with enhanced chemical stability: interplay between the N-terminal amino acid alkyl side chain and the cyclopropyl group of alpha-aminoacyl-l-cis-4,5-methanoprolinenitrile-based inhibitors.
Magnin DR, Robl JA, Sulsky RB, Augeri DJ, Huang Y, Simpkins LM, Taunk PC, Betebenner DA, Robertson JG, Abboa-Offei BE, Wang A, Cap M, Xin L, Tao L, Sitkoff DF, Malley MF, Gougoutas JZ, Khanna A, Huang Q, Han SP, Parker RA, Hamann LG.
J Med Chem (2004) 47 : 2587 -2598
PubMed 15115400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.33 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1627326 1 8.70
CHEMBL86677 1 8.40
CHEMBL86800 1 8.15
CHEMBL88949 1 8.15
CHEMBL1627303 1 8.10
CHEMBL89666 1 8.10
CHEMBL312855 1 7.96
CHEMBL313498 1 7.92
CHEMBL87153 1 7.92
CHEMBL86539 1 7.85
CHEMBL327435 1 7.82
CHEMBL430452 1 7.82
CHEMBL315434 1 7.60
CHEMBL88680 1 7.54
CHEMBL330523 1 7.19
CHEMBL328365 1 6.97
CHEMBL89272 1 6.87
CHEMBL89465 1 6.64
CHEMBL86334 1 5.79
CHEMBL327781 1 5.71
CHEMBL90223 1 5.12
CHEMBL89273 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1627326 Ki = 2.0 nM 8.70
CHEMBL86677 Ki = 4.0 nM 8.40
CHEMBL86800 Ki = 7.0 nM 8.15
CHEMBL88949 Ki = 7.0 nM 8.15
CHEMBL1627303 Ki = 8.0 nM 8.10
CHEMBL89666 Ki = 8.0 nM 8.10
CHEMBL312855 Ki = 11.0 nM 7.96
CHEMBL313498 Ki = 12.0 nM 7.92
CHEMBL87153 Ki = 12.0 nM 7.92
CHEMBL86539 Ki = 14.0 nM 7.85
CHEMBL327435 Ki = 15.0 nM 7.82
CHEMBL430452 Ki = 15.0 nM 7.82
CHEMBL315434 Ki = 25.0 nM 7.60
CHEMBL88680 Ki = 29.0 nM 7.54
CHEMBL330523 Ki = 65.0 nM 7.19
CHEMBL328365 Ki = 107.0 nM 6.97
CHEMBL89272 Ki = 135.0 nM 6.87
CHEMBL89465 Ki = 230.0 nM 6.64
CHEMBL86334 Ki = 1620.0 nM 5.79
CHEMBL327781 Ki = 1940.0 nM 5.71
CHEMBL90223 Ki = 7500.0 nM 5.12
CHEMBL89273 Ki = 10000.0 nM 5.00