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Assay Detail

CHEMBL900014

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

Binding
Inhibition of human DPP4
39
Total Activities
39
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 4 (CHEMBL284)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors.
Simpkins LM, Bolton S, Pi Z, Sutton JC, Kwon C, Zhao G, Magnin DR, Augeri DJ, Gungor T, Rotella DP, Sun Z, Liu Y, Slusarchyk WS, Marcinkeviciene J, Robertson JG, Wang A, Robl JA, Atwal KS, Zahler RL, Parker RA, Kirby MS, Hamann LG.
Bioorg Med Chem Lett (2007) 17 : 6476 -6480
PubMed 17937986 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 39 6.56 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL385517 SAXAGLIPTIN ANHYDROUS 4.0 1 9.22
CHEMBL391211 1 8.54
CHEMBL238024 1 8.00
CHEMBL238026 1 7.85
CHEMBL236479 1 7.55
CHEMBL236057 1 7.31
CHEMBL391186 1 6.95
CHEMBL238232 1 6.82
CHEMBL236480 1 6.57
CHEMBL238226 1 6.45
CHEMBL238014 1 6.28
CHEMBL236481 1 6.22
CHEMBL238225 1 6.14
CHEMBL238221 1 6.06
CHEMBL395184 1 6.00
CHEMBL238013 1 5.97
CHEMBL399411 1 5.85
CHEMBL238235 1 5.71
CHEMBL235225 1 5.52
CHEMBL391212 1 5.51
CHEMBL236310 1 5.49
CHEMBL236266 1 5.48
CHEMBL235868 1 5.44
CHEMBL395908 1 -
CHEMBL393575 1 -
CHEMBL235885 1 -
CHEMBL236097 1 -
CHEMBL236098 1 -
CHEMBL392467 1 -
CHEMBL392468 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL385517 SAXAGLIPTIN ANHYDROUS Ki = 0.6 nM 9.22
CHEMBL391211 Ki = 2.9 nM 8.54
CHEMBL238024 Ki = 10.0 nM 8.00
CHEMBL238026 Ki = 14.0 nM 7.85
CHEMBL236479 Ki = 28.0 nM 7.55
CHEMBL236057 Ki = 49.0 nM 7.31
CHEMBL391186 Ki = 112.0 nM 6.95
CHEMBL238232 Ki = 152.0 nM 6.82
CHEMBL236480 Ki = 270.0 nM 6.57
CHEMBL238226 Ki = 356.0 nM 6.45
CHEMBL238014 Ki = 530.0 nM 6.28
CHEMBL236481 Ki = 607.0 nM 6.22
CHEMBL238225 Ki = 731.0 nM 6.14
CHEMBL238221 Ki = 877.0 nM 6.06
CHEMBL395184 Ki = 1010.0 nM 6.00
CHEMBL238013 Ki = 1065.0 nM 5.97
CHEMBL399411 Ki = 1420.0 nM 5.85
CHEMBL238235 Ki = 1944.0 nM 5.71
CHEMBL235225 Ki = 3007.0 nM 5.52
CHEMBL391212 Ki = 3081.0 nM 5.51
CHEMBL236310 Ki = 3257.0 nM 5.49
CHEMBL236266 Ki = 3311.0 nM 5.48
CHEMBL235868 Ki = 3653.0 nM 5.44
CHEMBL235218 Ki > 10000.0 nM -
CHEMBL400230 Ki > 10000.0 nM -
CHEMBL412376 Ki > 10000.0 nM -
CHEMBL237090 Ki > 10000.0 nM -
CHEMBL395185 Ki > 10000.0 nM -
CHEMBL442704 Ki > 10000.0 nM -
CHEMBL236101 Ki > 10000.0 nM -
CHEMBL397052 Ki > 10000.0 nM -
CHEMBL236100 Ki > 10000.0 nM -
CHEMBL392468 Ki > 10000.0 nM -
CHEMBL392467 Ki > 10000.0 nM -
CHEMBL236098 Ki > 10000.0 nM -
CHEMBL236097 Ki > 10000.0 nM -
CHEMBL235885 Ki > 10000.0 nM -
CHEMBL393575 Ki > 10000.0 nM -
CHEMBL395908 Ki > 10000.0 nM -