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Assay Detail

CHEMBL2091655

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

Binding
Inhibition of human DPP4 expressed in baculovirus expression system using Gly-Pro-AMC substrate incubated or 30 mins by fluorescence based assay
32
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

Long-acting peptidomimetics based DPP-IV inhibitors.
Jadav P, Bahekar R, Shah SR, Patel D, Joharapurkar A, Kshirsagar S, Jain M, Shaikh M, Sairam KV.
Bioorg Med Chem Lett (2012) 22 : 3516 -3521
PubMed 22503246 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.10 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2086613 1 8.64
CHEMBL142703 VILDAGLIPTIN 4.0 1 8.49
CHEMBL2086614 1 8.42
CHEMBL77538 1 8.14
CHEMBL2086611 1 7.99
CHEMBL2086615 1 7.94
CHEMBL2086612 1 7.88
CHEMBL2086616 1 7.84
CHEMBL2086600 1 7.72
CHEMBL2086599 1 7.58
CHEMBL2086592 1 7.55
CHEMBL2086608 1 7.51
CHEMBL2086591 1 7.51
CHEMBL2086607 1 7.47
CHEMBL2086598 1 7.13
CHEMBL2086590 1 7.03
CHEMBL2086606 1 7.00
CHEMBL2086602 1 6.98
CHEMBL2086594 1 6.97
CHEMBL2086610 1 6.94
CHEMBL2086595 1 6.53
CHEMBL2086603 1 6.51
CHEMBL2086587 1 6.50
CHEMBL2086601 1 6.16
CHEMBL2086593 1 6.15
CHEMBL2086609 1 6.14
CHEMBL2086597 1 6.07
CHEMBL2086605 1 6.06
CHEMBL2086604 1 6.06
CHEMBL2086596 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2086613 IC50 = 2.3 nM 8.64
CHEMBL142703 VILDAGLIPTIN IC50 = 3.2 nM 8.49
CHEMBL2086614 IC50 = 3.8 nM 8.42
CHEMBL77538 IC50 = 7.2 nM 8.14
CHEMBL2086611 IC50 = 10.3 nM 7.99
CHEMBL2086615 IC50 = 11.6 nM 7.94
CHEMBL2086612 IC50 = 13.2 nM 7.88
CHEMBL2086616 IC50 = 14.3 nM 7.84
CHEMBL2086600 IC50 = 19.0 nM 7.72
CHEMBL2086599 IC50 = 26.0 nM 7.58
CHEMBL2086592 IC50 = 28.0 nM 7.55
CHEMBL2086608 IC50 = 31.0 nM 7.51
CHEMBL2086591 IC50 = 31.0 nM 7.51
CHEMBL2086607 IC50 = 34.0 nM 7.47
CHEMBL2086598 IC50 = 74.0 nM 7.13
CHEMBL2086590 IC50 = 93.0 nM 7.03
CHEMBL2086606 IC50 = 100.0 nM 7.00
CHEMBL2086602 IC50 = 104.0 nM 6.98
CHEMBL2086594 IC50 = 107.0 nM 6.97
CHEMBL2086610 IC50 = 116.0 nM 6.94
CHEMBL2086595 IC50 = 298.0 nM 6.53
CHEMBL2086603 IC50 = 311.0 nM 6.51
CHEMBL2086587 IC50 = 320.0 nM 6.50
CHEMBL2086601 IC50 = 694.0 nM 6.16
CHEMBL2086593 IC50 = 715.0 nM 6.15
CHEMBL2086609 IC50 = 723.0 nM 6.14
CHEMBL2086597 IC50 = 843.0 nM 6.07
CHEMBL2086605 IC50 = 863.0 nM 6.06
CHEMBL2086604 IC50 = 879.0 nM 6.06
CHEMBL2086596 IC50 = 869.0 nM 6.06
CHEMBL2086589 IC50 = 863.0 nM 6.06
CHEMBL2086588 IC50 = 890.0 nM 6.05