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Assay Detail

CHEMBL912993

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

Binding
Inhibition of Zucker rat DPP4
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.
Madar DJ, Kopecka H, Pireh D, Yong H, Pei Z, Li X, Wiedeman PE, Djuric SW, Von Geldern TW, Fickes MG, Bhagavatula L, McDermott T, Wittenberger S, Richards SJ, Longenecker KL, Stewart KD, Lubben TH, Ballaron SJ, Stashko MA, Long MA, Wells H, Zinker BA, Mika AK, Beno DW, Kempf-Grote AJ, Polakowski J, Segreti J, Reinhart GA, Fryer RM, Sham HL, Trevillyan JM.
J Med Chem (2006) 49 : 6416 -6420
PubMed 17034148 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 9.00 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386369 1 9.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386369 Ki = 1.0 nM 9.00