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Assay Detail

CHEMBL863902

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

Binding
Inhibition of human DPP4
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dipeptidyl peptidase 4 (CHEMBL284)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.
Qiao L, Baumann CA, Crysler CS, Ninan NS, Abad MC, Spurlino JC, Desjarlais RL, Kervinen J, Neeper MP, Bayoumy SS, Williams R, Deckman IC, Dasgupta M, Reed RL, Huebert ND, Tomczuk BE, Moriarty KJ.
Bioorg Med Chem Lett (2006) 16 : 123 -128
PubMed 16236500 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 7.07 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL199905 1 8.66
CHEMBL199614 1 8.51
CHEMBL199615 1 8.28
CHEMBL200347 1 7.89
CHEMBL199568 1 7.70
CHEMBL199922 1 7.58
CHEMBL77538 1 7.57
CHEMBL199881 1 7.47
CHEMBL380783 1 7.44
CHEMBL201268 1 7.20
CHEMBL199787 1 7.02
CHEMBL199735 1 6.80
CHEMBL199315 1 6.78
CHEMBL371757 1 6.77
CHEMBL199630 1 6.51
CHEMBL200119 1 6.44
CHEMBL199437 1 6.44
CHEMBL382281 1 6.33
CHEMBL381420 1 6.01
CHEMBL199790 1 5.94
CHEMBL199297 1 5.05
CHEMBL201391 1 -
CHEMBL381867 1 -
CHEMBL380760 1 -
CHEMBL199349 1 -
CHEMBL198131 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL199905 Ki = 2.2 nM 8.66
CHEMBL199614 Ki = 3.1 nM 8.51
CHEMBL199615 Ki = 5.3 nM 8.28
CHEMBL200347 Ki = 13.0 nM 7.89
CHEMBL199568 Ki = 20.0 nM 7.70
CHEMBL199922 Ki = 26.0 nM 7.58
CHEMBL77538 Ki = 27.0 nM 7.57
CHEMBL199881 Ki = 34.0 nM 7.47
CHEMBL380783 Ki = 36.0 nM 7.44
CHEMBL201268 Ki = 63.0 nM 7.20
CHEMBL199787 Ki = 96.0 nM 7.02
CHEMBL199735 Ki = 160.0 nM 6.80
CHEMBL199315 Ki = 166.0 nM 6.78
CHEMBL371757 Ki = 170.0 nM 6.77
CHEMBL199630 Ki = 310.0 nM 6.51
CHEMBL200119 Ki = 360.0 nM 6.44
CHEMBL199437 Ki = 360.0 nM 6.44
CHEMBL382281 Ki = 470.0 nM 6.33
CHEMBL381420 Ki = 980.0 nM 6.01
CHEMBL199790 Ki = 1160.0 nM 5.94
CHEMBL199297 Ki = 8900.0 nM 5.05
CHEMBL201391 Ki > 12800.0 nM -
CHEMBL381867 Ki > 12800.0 nM -
CHEMBL380760 Ki > 12800.0 nM -
CHEMBL199349 Ki > 12800.0 nM -
CHEMBL198131 Ki > 12800.0 nM -