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Assay Detail

CHEMBL988353

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Binding
Inhibition of human plasma DPP4
ChEMBL ↗
45
Total Activities
45
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of conformationally rigid 3-azabicyclo[3.1.0]hexane-derived dipeptidyl peptidase-IV inhibitors.
Sattigeri JA, Andappan MM, Kishore K, Thangathirupathy S, Sundaram S, Singh S, Sharma S, Davis JA, Chugh A, Bansal VS.
Bioorg Med Chem Lett (2008) 18 : 4087 -4091
PubMed 18602260 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 6.76 7.57
Ki 5 7.97 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL480903 — — 1 9.00
CHEMBL480716 — — 1 8.30
CHEMBL519435 — — 1 7.92
CHEMBL511125 — — 1 7.57
CHEMBL480530 — — 1 7.51
CHEMBL479538 — — 1 7.51
CHEMBL520434 — — 1 7.42
CHEMBL520266 — — 1 7.38
CHEMBL471956 — — 1 7.31
CHEMBL471960 — — 1 7.29
CHEMBL481288 — — 1 7.23
CHEMBL481177 — — 1 7.20
CHEMBL480705 — — 1 7.11
CHEMBL520575 — — 1 7.10
CHEMBL482261 — — 1 7.08
CHEMBL479736 — — 1 7.07
CHEMBL452998 — — 1 7.04
CHEMBL479794 — — 1 7.04
CHEMBL480712 — — 1 7.03
CHEMBL481669 — — 1 7.02
CHEMBL480155 — — 1 7.02
CHEMBL479567 — — 1 6.96
CHEMBL480914 — — 1 6.96
CHEMBL480942 — — 1 6.93
CHEMBL480324 — — 1 6.91
CHEMBL480781 — — 1 6.85
CHEMBL479983 — — 1 6.84
CHEMBL519265 — — 1 6.83
CHEMBL479381 — — 1 6.82
CHEMBL481290 — — 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL480903 — Ki = 1.0 nM 9.00
CHEMBL480716 — Ki = 5.0 nM 8.30
CHEMBL519435 — Ki = 12.0 nM 7.92
CHEMBL511125 — IC50 = 27.0 nM 7.57
CHEMBL480530 — Ki = 31.0 nM 7.51
CHEMBL479538 — IC50 = 31.0 nM 7.51
CHEMBL520434 — IC50 = 38.0 nM 7.42
CHEMBL520266 — IC50 = 42.0 nM 7.38
CHEMBL471956 — IC50 = 49.0 nM 7.31
CHEMBL471960 — IC50 = 51.0 nM 7.29
CHEMBL481288 — IC50 = 59.0 nM 7.23
CHEMBL481177 — IC50 = 63.0 nM 7.20
CHEMBL480705 — IC50 = 78.0 nM 7.11
CHEMBL520575 — Ki = 79.0 nM 7.10
CHEMBL482261 — IC50 = 84.0 nM 7.08
CHEMBL479736 — IC50 = 85.0 nM 7.07
CHEMBL452998 — IC50 = 91.0 nM 7.04
CHEMBL479794 — IC50 = 92.0 nM 7.04
CHEMBL480712 — IC50 = 93.0 nM 7.03
CHEMBL481669 — IC50 = 95.0 nM 7.02
CHEMBL480155 — IC50 = 95.0 nM 7.02
CHEMBL480914 — IC50 = 109.0 nM 6.96
CHEMBL479567 — IC50 = 110.0 nM 6.96
CHEMBL480942 — IC50 = 118.0 nM 6.93
CHEMBL480324 — IC50 = 123.0 nM 6.91
CHEMBL480781 — IC50 = 141.0 nM 6.85
CHEMBL479983 — IC50 = 146.0 nM 6.84
CHEMBL519265 — IC50 = 147.0 nM 6.83
CHEMBL479381 — IC50 = 153.0 nM 6.82
CHEMBL481290 — IC50 = 152.0 nM 6.82
CHEMBL479380 — IC50 = 165.0 nM 6.78
CHEMBL482262 — IC50 = 181.0 nM 6.74
CHEMBL480536 — IC50 = 186.0 nM 6.73
CHEMBL482104 — IC50 = 186.0 nM 6.73
CHEMBL480537 — IC50 = 221.0 nM 6.66
CHEMBL480154 — IC50 = 229.0 nM 6.64
CHEMBL479803 — IC50 = 422.0 nM 6.38
CHEMBL520921 — IC50 = 630.0 nM 6.20
CHEMBL519272 — IC50 = 1300.0 nM 5.89
CHEMBL480943 — IC50 = 1715.0 nM 5.77
CHEMBL480913 — IC50 = 2540.0 nM 5.59
CHEMBL471784 — IC50 = 3430.0 nM 5.46
CHEMBL471785 — IC50 = 3740.0 nM 5.43
CHEMBL509391 — IC50 = 3670.0 nM 5.43
CHEMBL480713 — IC50 > 10000.0 nM -