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Assay Detail

CHEMBL1218970

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

Binding
Inhibition of human recombinant DPP4 assessed as Gly-Pro-pNA cleavage
34
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors.
Meng W, Brigance RP, Chao HJ, Fura A, Harrity T, Marcinkeviciene J, O'Connor SP, Tamura JK, Xie D, Zhang Y, Klei HE, Kish K, Weigelt CA, Turdi H, Wang A, Zahler R, Kirby MS, Hamann LG.
J Med Chem (2010) 53 : 5620 -5628
PubMed 20684603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 8.73 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1215018 1 9.70
CHEMBL1215088 1 9.52
CHEMBL1214876 3 9.40
CHEMBL1215087 1 9.30
CHEMBL1215164 1 9.22
CHEMBL1215236 1 9.15
CHEMBL1215301 1 9.05
CHEMBL1215089 1 9.05
CHEMBL1215016 1 9.00
CHEMBL1215233 1 8.96
CHEMBL1215448 1 8.89
CHEMBL1215376 1 8.85
CHEMBL1215375 1 8.82
CHEMBL1215165 1 8.74
CHEMBL1215234 1 8.70
CHEMBL1215163 1 8.70
CHEMBL1214943 1 8.66
CHEMBL1214877 1 8.62
CHEMBL1215299 1 8.59
CHEMBL1215167 1 8.59
CHEMBL1214942 1 8.54
CHEMBL1214944 1 8.51
CHEMBL1215017 1 8.51
CHEMBL1215235 1 8.49
CHEMBL1215166 1 8.42
CHEMBL1215300 1 8.40
CHEMBL1215373 1 8.33
CHEMBL1214945 1 8.30
CHEMBL1215302 1 8.30
CHEMBL1215374 1 8.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1215018 Ki = 0.2 nM 9.70
CHEMBL1215088 Ki = 0.3 nM 9.52
CHEMBL1214876 Ki = 0.4 nM 9.40
CHEMBL1215087 Ki = 0.5 nM 9.30
CHEMBL1215164 Ki = 0.6 nM 9.22
CHEMBL1214876 Ki = 0.7 nM 9.15
CHEMBL1215236 Ki = 0.7 nM 9.15
CHEMBL1215301 Ki = 0.9 nM 9.05
CHEMBL1215089 Ki = 0.9 nM 9.05
CHEMBL1215016 Ki = 1.0 nM 9.00
CHEMBL1215233 Ki = 1.1 nM 8.96
CHEMBL1215448 Ki = 1.3 nM 8.89
CHEMBL1215376 Ki = 1.4 nM 8.85
CHEMBL1215375 Ki = 1.5 nM 8.82
CHEMBL1215165 Ki = 1.8 nM 8.74
CHEMBL1215234 Ki = 2.0 nM 8.70
CHEMBL1215163 Ki = 2.0 nM 8.70
CHEMBL1214943 Ki = 2.2 nM 8.66
CHEMBL1214877 Ki = 2.4 nM 8.62
CHEMBL1215299 Ki = 2.6 nM 8.59
CHEMBL1215167 Ki = 2.6 nM 8.59
CHEMBL1214942 Ki = 2.9 nM 8.54
CHEMBL1215017 Ki = 3.1 nM 8.51
CHEMBL1214944 Ki = 3.1 nM 8.51
CHEMBL1215235 Ki = 3.2 nM 8.49
CHEMBL1215166 Ki = 3.8 nM 8.42
CHEMBL1215300 Ki = 4.0 nM 8.40
CHEMBL1215373 Ki = 4.7 nM 8.33
CHEMBL1215302 Ki = 5.0 nM 8.30
CHEMBL1214945 Ki = 5.0 nM 8.30
CHEMBL1215374 Ki = 5.4 nM 8.27
CHEMBL1215090 Ki = 6.6 nM 8.18
CHEMBL1215015 Ki = 8.7 nM 8.06
CHEMBL1214876 Ki = 11.7 nM 7.93