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Assay Detail

CHEMBL3074800

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

Binding
Inhibition of dipeptidyl peptidase 4 (unknown origin)
37
Total Activities
37
Compounds Tested
2
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

Computational studies on structurally diverse dipeptidyl peptidase IV inhibitors: an approach for new antidiabetic drug development
Patel B, Ghate M
Med Chem Res (2013) 22 : 4505 -4521
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.71 10.00
Ki 8 8.50 9.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34062 1 10.00
CHEMBL1229820 1 9.30
CHEMBL1230804 1 9.09
CHEMBL237500 LINAGLIPTIN 4.0 1 9.00
CHEMBL1214943 1 8.66
CHEMBL400841 1 8.64
CHEMBL225210 1 8.49
CHEMBL1230909 1 8.47
CHEMBL1230826 1 8.42
CHEMBL1234200 1 8.40
CHEMBL237337 1 8.37
CHEMBL237997 1 8.32
CHEMBL226396 6-CHLOROGUANINE 1 8.30
CHEMBL1232261 1 8.28
CHEMBL591118 CARMEGLIPTIN 2.0 1 8.17
CHEMBL1230763 1 8.17
CHEMBL1233461 1 8.15
CHEMBL272114 1 8.10
CHEMBL1185242 1 7.92
CHEMBL515387 GOSOGLIPTIN 4.0 1 7.89
CHEMBL227954 1 7.89
CHEMBL1229855 1 7.80
CHEMBL1230015 1 7.72
CHEMBL233360 1 7.68
CHEMBL1229644 1 7.66
CHEMBL2298396 1 7.64
CHEMBL250787 1 7.60
CHEMBL452289 1 7.50
CHEMBL1197118 1 7.38
CHEMBL1230044 1 7.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34062 IC50 = 0.1 nM 10.00
CHEMBL1229820 IC50 = 0.5 nM 9.30
CHEMBL1230804 Ki = 0.82 nM 9.09
CHEMBL237500 LINAGLIPTIN IC50 = 1.0 nM 9.00
CHEMBL1214943 Ki = 2.2 nM 8.66
CHEMBL400841 IC50 = 2.3 nM 8.64
CHEMBL225210 Ki = 3.2 nM 8.49
CHEMBL1230909 Ki = 3.4 nM 8.47
CHEMBL1230826 Ki = 3.8 nM 8.42
CHEMBL1234200 Ki = 4.0 nM 8.40
CHEMBL237337 IC50 = 4.3 nM 8.37
CHEMBL237997 IC50 = 4.8 nM 8.32
CHEMBL226396 6-CHLOROGUANINE IC50 = 5.0 nM 8.30
CHEMBL1232261 Ki = 5.3 nM 8.28
CHEMBL1230763 Ki = 6.7 nM 8.17
CHEMBL591118 CARMEGLIPTIN IC50 = 6.8 nM 8.17
CHEMBL1233461 IC50 = 7.0 nM 8.15
CHEMBL272114 IC50 = 8.0 nM 8.10
CHEMBL1185242 IC50 = 12.0 nM 7.92
CHEMBL227954 IC50 = 13.0 nM 7.89
CHEMBL515387 GOSOGLIPTIN IC50 = 12.9 nM 7.89
CHEMBL1229855 IC50 = 16.0 nM 7.80
CHEMBL1230015 IC50 = 19.0 nM 7.72
CHEMBL233360 IC50 = 21.0 nM 7.68
CHEMBL1229644 IC50 = 22.0 nM 7.66
CHEMBL2298396 IC50 = 23.0 nM 7.64
CHEMBL250787 IC50 = 25.0 nM 7.60
CHEMBL452289 IC50 = 32.0 nM 7.50
CHEMBL1197118 IC50 = 42.0 nM 7.38
CHEMBL1230044 IC50 = 65.0 nM 7.19
CHEMBL1194345 IC50 = 67.0 nM 7.17
CHEMBL513425 IC50 = 70.0 nM 7.16
CHEMBL218289 IC50 = 84.0 nM 7.08
CHEMBL425584 IC50 = 90.0 nM 7.05
CHEMBL1186902 IC50 = 223.0 nM 6.65
CHEMBL1236897 IC50 = 2000.0 nM 5.70
CHEMBL257036 IC50 = 30000.0 nM 4.52